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Neuroscience
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An internal standard for the quantification of arachidonoyl ethanolamide
Arachidonoyl ethanolamide-d4 (AEA-d4) contains four deuterium atoms at the hydroxyethyl 1,1',2, and 2' positions. It is intended for use as an internal standard for the quantification of AEA by GC- or LC-mass spectrometry.
For immunochemical detection of CB1 receptor
An internal standard for the quantification of 8-iso prostaglandin F2α
8-iso PGF2α-d4 contains four deuterium atoms at the 3, 3', 4, and 4' positions. It is intended for use as an internal standard for the quantification of 8-iso PGF2α by GC- or LC-mass spectrometry.
A potent inhibitor of FAAH
An internal standard for the quantification of 2-arachidonoyl glycerol
2-Arachidonoyl glycerol-d8 (2-AG-d8) contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14, and 15 positions of the arachidonic acid moiety. It is intended for use as an internal standard for the quantification of 2-AG by GC- or LC-mass spectrometry.
An aspirin-induced DHA metabolite
17(R)-HDoHE is the primary oxygenation product of DHA when exposed to aspirin-inhibited cyclooxygenase-2. 17(R)-HDoHE serves as a precursor to resolvins and has intrinsic biological activity, such as the inhibition of TNFα-induced IL-1β expression in human glioma cells.
An endocannabinoid discovered during a lipidomics survey
N-arachidonoyl taurine, a prominent N-acyl taurine, activates both TRPV1 and TRPV4 with EC50 values of 28 and 21 µM, respectively.
A highly purified, active enzyme preparation
One unit of enzyme produces one µmole of prostaglandin D2 (PGD2)/min at 25°C in 100 mM Tris-HCl buffer, pH 8.0, containing 1 mM GSH, 1 mg/ml γ-globulin, and 40 µM PGH2
An internal standard for the quantification of arachidonoyl ethanolamide
AEA-8 contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14, and 15 positions. It is intended for use as an internal standard for the quantification of AEA by GC- or LC-mass spectrometry.
Specifically measures the octanoylated active form of Ghrelin
Ghrelin, an endogenous ligand for the growth hormone secretagogue receptor, is synthesized principally in the stomach. It stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. The peptide consists of 28 amino acids, with an octanoylation of the serine-3 residue, which is necessary for biological activity. Ghrelin is present in the peripheral circulation in two forms: acylated and non-acylated. This EIA kit specifically measures the acylated form of ghrelin.
A fluorescent substrate for the anandamide transporter
CAY10455 is a labeled analog of AEA that is non-fluorescent when outside the cell. Upon transport into the cell interior, it is cleaved by esterases to give a bright fluorescence at 530 nm. CAY10455 uptake into C6 glioma cells is inhibited by AEA and its analogs, and conversely CAY10455 inhibits the uptake of tritiated AEA, indicating that they compete for the AEA transporter.
An endocannabinoid found in porcine brain
Arachidonoyl amides of both amino acids and neurotransmitters such as dopamine have been previously reported in the literature. N-Arachidonoyl-L-serine (ARA-S) is one such recently isolated endocannabinoid with an unusual activity profile. ARA-S does not bind to central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors or vanilloid receptor 1 (VR1). Like cannabidiol, ARA-S (5 mg/kg) antagonizes the hypotensive effects of a 10 mg/kg IV bolus of abnormal cannabidiol (Abn-CBD) in an anesthetized rat blood pressure model. However, similar to Abn-CBD, ARA-S relaxes isolated rat mesenteric arteries and abdominal aorta as well as increases phosphorylation of Akt and mitogen-activated protein kinase (MAPK) in HUVEC. The precise mechanisms of action by ARA-S and Abn-DBD in various vascular preparations appears to be different and requires further investigation.
Arachidonoyl ethanolamide (AEA) is the ethanolamine amide of arachidonic acid, first isolated from porcine brain. AEA is an endogenous cannabinoid neurotransmitter that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. AEA inhibits the specific binding of [3H]-HU-243 to synaptosomal membranes with a Ki value of 52 nM, compared to 46 nM for Δ9-THC.
A fully saturated anandamide analog
Arachidoyl ethanolamide is one of the saturated fatty acyl ethanolamides devoid of classical (CB1/CB2) activity. Arachidoyl ethanolamide does not bind to the murine CB1 receptor and does not compete with anandamide as a substrate for the endocannabinoid hydrolytic enzyme fatty acid amide hydrolase. Non-CB receptor-mediated pharmacology of the saturated ethanolamides is still being elucidated.
A cannabidiol analog with antiproliferative activity
HU-331 is a hydroxylquinone cannabidiol analog that exhibits potent antineoplastic activity on a variety of human cancer cell lines. It effectively inhibits the growth of human Raji and Jurkat lymphoma cells in vitro with an EC50 of approximately 0.2 µg/ml and an EC80 of 1.56 µg/ml. HU-331 also inhibits the growth of HT-29 colon carcinoma cells, which have been inoculated into nude mice, by more than 50% at a dose of 5 mg/kg.
A potent acetylcholinesterase inhibitor
Tacrine is an amino acridine compound that inhibits acetylcholinesterase (AChE), and has been proposed as a clinical treatment for Alzheimer’s disease. bis(7)-Tacrine is a tacrine dimer, linked via a 7-carbon alkyl spacer. It inhibits AChE with an IC50 of 0.40 nM, making it more than 1,000 times more potent than tacrine. bis(7)-Tacrine also protects against hydrogen peroxide induced apoptosis in rat pheochromocytoma cells.
A potent, selective FAAH inhibitor
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. CAY10435 is a selective, potent inhibitor of rat FAAH exhibiting a Ki value of 0.57 nM. Using a proteonomics approach, CAY10435 was screened against the serine hydrolase family of enzymes, of which FAAH is a member. In this assay, CAY10435 exhibited IC50 values of 0.81 nM, 83 nM, and 50 µM for FAAH, triacylglycerol hydrolase (TGH), and an uncharacterized hydrolase (KIAA1363), respectively.
An amino-acyl endocannabinoid
N-Oleoyl taurine is an amino-acyl endocannabinoid isolated from rat brain that may activate TRPV1 and TRPV4.
A potent capsaicin/TRPV1 antagonist
CAY10448 is an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 of approximately 10 nM.
A hydrolysis-resistant endocannabinoid analog that inhibits AEA cellular uptake
AM1172 is an endocannabinoid analog specifically designed to be a potent and selective inhibitor of AEA uptake that is resistant to FAAH hydrolysis. Structurally, AM1172 is the “reversed” isomer of AM404, constructed using arachidonyl amine; this may account for its metabolic stability. In murine cortical neurons, AM1172 blocked the uptake of tritiated AEA with an EC50 of about 1.5 µM.
An analog of O-1918, a selective antagonist of a non-CB1/CB2 receptor
O-1602 is a cannabidiol analog with close structural similarity to O-1918 which is a selective antagonist of abnormal cannabidiol at the non-CB1/CB2 endothelial receptor. O-1918 does not bind to CB1 or CB2 receptors at concentrations up to 30 µM and inhibits the vasorelaxant effects of abnormal cannabidiol in vitro and in whole animals. The biological activity of O-1821 has not been reported.
An endocannabinoid analog that inhibits FAAH and has analgesic activity
Oleoyl ethyl amide (OEtA) has potent FAAH inhibitory activity (IC50 5.25 nM in rat brain homogenates) but does not inhibit acidic PEAase or bind to CB1 or CB2 receptors. OEtA is therefore a selective FAAH inhibitor with potential analgesic and anxiolytic activity.
A saturated N-acylethanolamide for cannabinoid research
Docosanoyl ethanolamide is a saturated N-acylethanolamide. Non-cannabinoid receptor-mediated pharmacology of the saturated ethanolamides is still being elucidated. Other studies indicate they may have a role in the functioning of ion channels.
A colorimetric FAAH substrate used for enzyme activity measurement
N-Decanoyl p-nitroaniline (DepNA) is one of several nitroaniline fatty acid amides which can be used to measure fatty acid amide hydrolase (FAAH) activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its endogenous substrate anandamide (AEA). It also will hydrolyze fatty acid amides with fewer carbons and fewer double bonds than arachidonate. Exposure of DepNA to FAAH activity results in the release of the yellow colorimetric dye p-nitroaniline (ε = 13,500 at 410 nm). This allows the fast and convenient measurement of FAAH activity using a 96 well plate spectrophotometer.
An amino-acyl endocannabinoid
N-Palmitoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling. Its function is currently under investigation.
An antioxidant metabolite of melatonin
AFMK is a melatonin metabolite first identified in rat brain. AFMK has antioxidant and free radical scavenging activities in several experimental models. AFMK may also be measured in plasma as an index of melatonin synthesis and metabolism.
An amino-acyl endocannabinoid
N-Stearoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling.
A selective, potent FAAH inhibitor
PF-750 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values 0.6 and 0.016 µM when preincubated with recombinant human FAAH for 5 and 60 minutes, respectively. Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.
A selective, potent FAAH inhibitor
PF-622 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values 0.99 and 0.033 µM when preincubated with human recombinant FAAH for 5 and 60 minutes, respectively. Activity-based profiling of various human and murine tissue proteome samples revealed that PF-622 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.
A deuterated internal standard for a predominant isoprostane isomer
8,12-iso-iPF2α-VI-d11 contains 11 deuterium atoms at the 16, 16', 17, 17', 18, 18', 19, 19', 20, 20, and 20 positions. It is intended for use as an internal standard for the quantification of 8,12-iso-iPF2α-VI by GC- or LC-mass spectrometry. The relative abundance of deuterium atoms incorporated into each molecule has not been determined. Cayman certifies that less that 1% of the product has no deuterium incorporation (<1% d0).
An internal standard for the quantification of prostaglandin D2
PGD2-d4 contains four deuterium atoms at the 3, 3', 4, and 4' positions. It is intended for use as an internal standard for the quantification of PGD2 by GC- or LC-mass spectrometry.
Highly purified, active enzyme preparation
One unit of enzyme produces one µmole of prostaglandin D2 (PGD2)/min at 25°C in 100 mM Tris-HCl buffer, pH 8.0, containing 1 mM GSH, 1 mg/ml γ-globulin, and 40 µM PGH2
An analog of O-1918, a selective antagonist of a non-CB1/CB2 receptor
O-1821 is a cannabidiol analog with close structural similarity to O-1918 which is a selective antagonist of abnormal cannabidiol at the non-central cannabinoid (CB1)/peripheral cannabinoid (CB2) receptors endothelial receptor. O-1918 does not bind to CB1 or CB2 receptors at concentrations up to 30 µM and inhibits the vasorelaxant effects of abnormal cannabidiol in vitro and in whole animals. The biological activity of O-1821 has not been reported.
A selective anandamide uptake inhibitor
VDM11 is an anandamide transport inhibitor with essentially no activity on either the central cannabinoid receptor (CB1), peripheral cannabinoid receptor (CB2), or the vanilloid receptor 1 (VR1). However, VDM11 inhibits FAAH and monoacylglycerol lipase (MAGL) and may act as an alternative FAAH substrate. At a concentration of 3 µM, VDM11, like AM404, inhibits glutamergic synaptic transmission between hippocampal neurons. The mechanism of this effect may be a direct action on sodium channels. Thus, the use of anandamide analogs as uptake inhibitors and interpretation of the results must be undertaken with care.
A CB2 receptor antagonist
AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 µM and 31.2 nM, respectively. AM630 behaves as an inverse agonist at CB2 receptors, attenuating the antinociceptive effects of a number of cannabinoids, and as a weak partial agonist at CB1 receptors.
Designed for the convenient, precise quantification of DHA
The docosahexaenoic acid (DHA) Quant-PAK has been designed for the convenient, precise quantification of DHA by GC- or LC-MS. It includes a 50 µg vial of DHA-d5 and a precisely weighed vial of unlabeled DHA, with the precise weight (2-4 mg) indicated on the vial. This unlabeled DHA can be used to quantify the DHA-d5 standard by constructing a standard curve of peak intensity ratios (deuterated versus unlabeled).
Precursor of oleoyl ethanolamide
Glycerophospho-N-oleoyl ethanolamine is the precursor of oleoyl ethanolamide (OEA). OEA is an endogenous, potent agonist for PPARα, exhibiting an EC50 value of 120 nM in a transactivation assay. Systemic administration of OEA suppresses food intake and reduces weight gain in rats (10 mg/kg intraperitoneally) and PPARα wild-type mice, but not in PPARα knockout mice. Like AEA, OEA is metabolized by fatty acid amide hydrolase (FAAH).
Precursor for palmitoyl ethanolamide
Glycerophospho-N-palmitoyl ethanolamine (GP-NPEA) is the metabolic precursor of palmitoyl ethanolamide (PEA). PEA is an endogenous cannabinoid found in brain, liver, and other mammalian tissues, that has potent anti-inflammatory activity in vivo. PEA has low affinity for peripheral cannabinoid (CB2) and no appreciable affinity for central cannabinoid (CB1), suggesting that its efficacy is through a different receptor.
Positive control for Western blotting
A potent agonist of CB1 and CB2
WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 3.3 and 62.3 nM for human recombinant CB1 and CB2 receptors, respectively. In primary cultures of rat cerebral cortex neurons, WIN 55212-2 (mesylate) (0.01-100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve. This effect at a concentration of 1 nM was fully counteracted by SR141716A (10 nM), by decreasing Ca2+ concentrations below 0.2 mM, and by the IP3 receptor antagonist xestospongin C at 1 µM. WIN 55212-2 (mesylate) induces release of the proinflammatory neuropeptide CGRP from trigeminal ganglion (TG) neurons in a calcium-dependent manner with an EC50 of 26 µM. In addition, WIN 55212-2 (mesylate)-evoked CGRP release is not stereospecific, as the CB receptor-inactive enantiomer WIN 55212-3 also stimulates CGRP exocytosis.
An internal standard for the quantification of palmitoyl ethanolamide
Palmitoyl ethanolamide-d4 (PEA-d4) contains four deuterium atoms at the 7, 7', 8, and 8' positions. It is intended for use as an internal standard for the quantification of PEA by GC- or LC-mass spectrometry.
An internal standard for the quantification of oleoyl ethanolamide
Oleoyl ethanolamide-d2 (OEA-d2) contains two deuterium atoms at the 11 position. It is intended for use as an internal standard for the quantification of OEA by GC- or LC-mass spectrometry.
An agonist of CB1 and CB2
(−)-CP 55,940 is a potent, non-selective cannabinoid (CB) receptor agonist with Ki values of 0.58 and 0.69 nM for human recombinant CB1 and CB2, respectively. It is a commonly used reference molecule in CB research and is considerably more potent than Δ9-THC in both behavioral tests and in receptor binding assays.
An internal standard for the quantification of 2-arachidonoyl glycerol
2-Arachidonoyl glycerol-d5 (2-AG-d5) contains five deuterium atoms at the 1, 1, 2, 3, and 3 positions of the glycerol moiety. It is intended for use as an internal standard for the quantification of 2-AG by GC- or LC-mass spectrometry.
An inhibitor of voltage-gated calcium channels
SKF-96365 inhibits the receptor-mediated influx of calcium via voltage-gated calcium channels with an IC50 value of approximately 10 µM. It inhibits the acetylcholine-induced depolarization of circular smooth muscle in a dose-dependent manner at 3-50 µM. SKF-96365 can distinguish receptor-mediated release in platelets and neutrophils from the calcium release from internal stores. However, it does not distinguish between receptor-mediated and voltage-gated release.
A selective antagonist of CB1
(±)-SLV 319 is the mixture of the central cannabinoid (CB1) receptor antagonist SLV 319 and its distomer, SLV 319 (+)-enantiomer. SLV 319 is a potent and selective CB1 receptor antagonist with Ki values of 7.8 and 7,943 nM for CB1 and peripheral cannabinoid (CB2), respectively. SLV 319 is less lipophilic (log P = 5.1) and therefore more water soluble than other known CB1 receptor ligands.
A selective receptor agonist of CB2
JWH 015 is a selective aminoalkylindole peripheral cannabinoid (CB2) receptor agonist with Ki values of 13.8 and 383 nM for human recombinant CB2 and CB1 receptors, respectively. Using Theiler’s murine encephalomyelitis virus as a model for human multiple sclerosis (MS), treatment with WIN 55212-2, ACEA, and JWH 015 significantly improved the neurological deficit of established disease. JWH 015 was shown to reduce microglial activation, abrogate antigen expression, and decrease the number of CD4+ infiltrating T-cells in the spinal cord. In addition, JWH 015 reduces IFN-γ-induced up-regulation of CD40 expression in mouse microglial cells by interfering with the JAK/STAT1 pathway.
For immunochemical analysis of Cu/Zn SOD
A selective antagonist of CB1
(S)-SLV 319 is a potent and selective CB1 receptor antagonist with Ki values of 7.8 and 7,943 nM for CB1 and peripheral cannabinoid (CB2), respectively. (S)-SLV 319 is less lipophilic (log P = 5.1) and therefore more water soluble than other known CB1 receptor ligands.
A CB2 selective receptor agonist
L-759,633 is a high-affinity peripheral cannabinoid receptor (CB2)-selective agonist with Ki values of 6.4 and 1043 nM for CB2 and central cannabinoid (CB1) receptors, respectively. L-759,633 inhibits forskolin-stimulated cyclic AMP production in CHO cells transfected with CB2 or CB1 receptors with IC50 values of 8.1 nM and 10 µM, respectively.
A 'click chemistry' probe for FAAH
JP104 is an irreversible fatty acid amide hydrolase (FAAH) inhibitor of the carbamate class with an IC50 of 7.3 nM for the human recombinant enzyme when tested using radiolabeled oleamide as the substrate. The alkyl derivative on JP104 reacts with azide-modified reporter tags, such as azido-rhodamine or azido-biotin, for visualization of JP104 bound to FAAH in vivo.
SC-19220 is a dibenzoxazepine which acts as a selective antagonist of prostaglandin E2 (PGE2) at the EP1 receptor. At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach. SC-19220 acts as a PGE2 antagonist in the EP1 receptor mediated contraction of guinea pig trachea. SC-19220 displaces radiolabeled PGE2 from the cloned human EP1 receptor with an IC50 of 6.7 µM and exhibits no binding at the human EP2 receptor. It binds very weakly and shows no selectivity for the mouse EP1 receptor, suggesting species differences between the human and mouse EP1 receptors.
For immunochemical detection of the IP receptor
An approved antiepileptic drug
Gabapentin (Neurontin®) is a γ-aminobutyric acid (GABA) analogue that acts as an anticonvulsant with proven analgesic effects in various neuropathic pain syndromes such as Complex Regional Pain Syndrome type one (CRPS 1). It is also prescribed to multiple sclerosis patients to control dysesthesias and may be useful in reducing neuropathic pain caused by cancer and HIV infection. It does not bind to GABA receptors, does not influence neural uptake of GABA, and does not inhibit the GABA-metabolizing enzyme, GABA transaminase. Unlike GABA, which does not pass through the blood brain barrier, gabapentin penetrates into the central nervous system and binds to the α2δ-type voltage-gated calcium channels. The mechanism for the analgesic and anticonvulsant effects of gabapentin are not known.
A potent, irreversible FAAH inhibitor
JP83 is an irreversible fatty acyl amide hydrolase (FAAH) inhibitor of the carbamate class with an IC50 of 14 nM for the human recombinant enzyme when tested using radiolabeled oleamide as the substrate.
A selective agonist of GPR119
PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to oleoyl ethanolamide (OEA) at both recombinant murine and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively). Systemic administration of PSN632408 (30 mg/kg intraperitoneally) suppresses food intake, reduces weight gain, and white adipose tissue deposition in rats. These data suggest that PSN632408 may be useful as a therapeutic agent for the treatment of obesity.
A chromogenic substrate for measurement of monoacylglycerol lipase activity
Arachidonoyl-1-thio-glycerol is a thioester substrate analog of 2-arachidonoyl glycerol that can be utilized for the measurement of monoacylglycerol lipase (MGL) activity. Hydrolysis of the thioester bond by MGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB (Ellman’s reagent) resulting a yellow product with an absorbance maximum at 412 nm.
A convenient fluorescence-based method for screening FAAH inhibitors
Cayman’s FAAH Inhibitor Screening Assay Kit provides a convenient fluorescence-based method for screening FAAH inhibitors. FAAH hydrolyzes AMC-arachidonoyl amide resulting in the release of the fluorescent product, 7-amino-4-methylcoumarin (AMC). The fluorophore can be easily analyzed using an excitation wavelength of 340-360 nm and an emission wavelength of 450-465 nm.
An A3 adenosine receptor antagonist
CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells. However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated.
A potential cytochrome P450 metabolite of AEA
(±)11(12)-EET ethanolamide is a potential cytochrome P450 (CYP450) metabolite of AEA, although specific stereochemistry rather than a racemic mixture would likely ensue from enzymatic metabolism. CYP450 metabolism of AEA may be particularly relevant under conditions of FAAH inhibition. Evidence for the formation of 11(12)-EET ethanolamide in vivo has not been documented.
A potential cytochrome P450 metabolite of AEA
(±)14(15)-EET ethanolamide is a potential cytochrome P450 (CYP450) metabolite of arachidonoyl ethanolamide (AEA), although specific stereochemistry rather than a racemic mixture would likely ensue from enzymatic metabolism. CYP450 metabolism of AEA may be particularly relevant under conditions of fatty acid amide hydrolase inhibition. Evidence for the formation of (±)14(15)-EET ethanolamide in vivo has not been documented.
2-Arachidonoyl glycerol (2-AG) is an endogenous agonist of the CB1 receptor. Unlike anandamide, 2-AG is present at relatively high levels in the central nervous system; it is the most abundant molecular species of monoacylglycerol found in rat brain. Formation of 2-AG is calcium-dependent and is mediated by the activities of PLC and DAG lipase. 2-AG acts as a full agonist at the CB1 receptor. At a concentration of 0.3 nM, 2-AG induces a rapid, transient increase in intracellular free calcium in NG108-15 neuroblastoma X glioma cells through a CB1 receptor-dependent mechanism. 2-AG is metabolized in vitro by MAG lipase and fatty acid amide hydrolase, with MAG lipase likely being the principle metabolizing enzyme in vivo.
Specifically measures the octanolyated active form of Ghrelin
Ghrelin, an endogenous ligand for the growth hormone secretagogue receptor, is synthesized principally in the stomach. It stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. The peptide consists of 28 amino acids, with an octanoylation of the serine-3 residue, which is necessary for biological activity. Ghrelin is present in the peripheral circulation in two forms: acylated and non-acylated. This EIA kit specifically measures the acylated form of ghrelin. This EIA is based on a double-antibody sandwich technique. The wells of the plate supplied with the kit are coated with a monoclonal antibody specific to the C-terminal part of ghrelin. This antibody will bind to any ghrelin introduced into the wells (standard or sample). The AChE - Fab' conjugate which recognizes the N-terminal part of acylated ghrelin is also added to the wells. This allows the two antibodies to form a sandwich by binding on different parts of the human acylated ghrelin. Each kit contains ghrelin (acylated) AChE-Fab' conjugate, human acylated ghrelin standard, human acylated ghrelin quality control, Ellman’s reagent, EIA buffer, wash buffer, Tween 20, plates pre-coated with anti-ghrelin mouse monoclonal antibody, and complete instructions.
Designed for the convenient, precise quantification of Prostaglandin D2 Ethanolamide
Designed for the convenient, precise quantification of Prostaglandin D2
Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. Mastocytosis patients produce excessive amounts of PGD2, which causes vasodilation, flushing, hypotension, and syncopal episodes. PGD2 is also produced in the brain via an alternative pathway involving a soluble, secreted PGD-synthase also known as β-trace. In the brain, PGD2 produces normal physiological sleep and lowering of body temperature. Further pharmacological actions include inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 inhibits human ovarian tumor cell proliferation with an IC50 value of 6.8 µM.
Designed for the convenient, precise quantification of Prostaglandin Ethanolamide E2
Prostaglandin E2 ethanolamide (PGE2-EA) is an analog of PGE2 with improved water solubility and stability. PGE2-EA acts as an agonist with all four known EP receptor subtypes, but with an affinity that is significantly reduced compared to PGE2. PGE2 ethanolamide is produced by HCA-7 cells treated with arachidonoyl ethanolamide (AEA). The physiologic relevance of PGE2 ethanolamide is not yet established.
A selective inhibitor of ABHD6
α/β-Hydrolase domain 6 (ABHD6) is a serine hydrolase that is highly expressed in mammalian brain. This enzyme catalyzes the hydrolysis of the endocannabinoid 2-arachidonoyl glycerol (2-AG). WWL70 is a selective inhibitor of ABHD6 with an IC50 value of 70 nM.
A potent CB1 receptor antagonist
AVE-1625 is a highly potent, selective antagonist for the CB1 receptor with Ki values of 0.16-0.44 nM. At 1-3 mg/kg, AVE-1625 significantly improves the performance of rodents in working memory tasks. At 30 mg/kg, AVE-1625 reduces caloric intake by more than 50% of controls and significantly increases lipolysis from fat tissues and reduces hepatic glycogen levels in rodents.
A selective inhibitor of monoglycerol lipase
URB602 is a selective inhibitor of monoglycerol lipase (MGL), exhibiting an IC50 of 28 µM for the rat brain enzyme. It does not inhibit fatty acid amide hydrolase at concentrations up to 100 µM, or other lipid metabolizing enzymes such as diacylglycerol lipase or cyclooxygenase-2. Inhibition of 2-arachidonoyl glycerol hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.
A potent water-soluble cannabinoid receptor agonist
O-2545 is a potent water-soluble agonist of central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors with Ki values of 1.5 and 0.32 nM, respectively. When dissolved in saline, O-2545 was highly efficacious in murine behavioral models when administered either intravenously or intracerebroventricularly.
A selective CB2 receptor agonist
HU-308 is a potent, selective agonist for the peripheral cannabinoid (CB2) receptor. The Ki for CB1 is >10 µM, while the Ki for CB2 is approximately 20 nM. When administered to whole animals, HU-308 elicits hypotensive, analgesic, and anti-inflammatory activity, but none of the behavioral tetrad of psychomotor responses characteristic of the phenolic components of hemp, such as Δ9-THC.
A bioactive precursor of 17(S)-Resolvins
17(S)-HDoHE is a primary mono-oxygenation product of docosahexaenoic acid in human whole blood, human leukocytes, and murine brain. 17(S)-HDoHE serves as a precursor to 17(S)-resolvins and has intrinsic biological activity, such as the inhibition of TNFα-induced interleukin-1β expression in human glioma cells and inhibition of TNFα-induced leukocyte trafficking to the murine air pouch.
A selective caspase 1/ICE inhibitor
N-Ac-Tyr-Val-Ala-Asp-chloromethyl ketone (Ac-YVAD-CMK) is a selective, irreversible inhibitor of interleukin-1β converting enzyme (ICE; Caspase-1). Ac-YVAD-CMK is neuroprotective in a rat model of cerebral ischemia.
For immunochemical analysis of NAPE-PLD
To be used in conjunction with Cayman’s NAPE-PLD polyclonal antibody (Catalog No. 10005430) to block protein-antibody complex formation during immunochemical analysis of NAPE-PLD.
A DHA epoxygenase metabolite
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as 14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) have been little studied relative to arachidonate epoxygenase metabolites. 19(20)-EpDPE is a DHA epoxygenase metabolite, derived via epoxidation of the ω-3 double bond of DHA. The EDHF activity of 19(20)-EpDPE has not yet been determined. The epoxygenase metabolites of DHA have also been detected in a murine inflammation model.
Positive control for western blotting
An endocannabinoid analog that potentiates AEA activity
An internal standard for the quantification of prostaglandin D2
PGD2-d9 contains nine deuterium atoms at the 17, 17', 18, 18', 19, 19', 20, 20, and 20 positions. It is intended for use as an internal standard for the quantification of PGD2 by GC- or LC-mass spectrometry.
An antioxidant, anti-inflammatory cannabinoid
HU-211 is a synthetic terpene-based cannabinoid devoid of central cannabinoid (CB1) and peripheral cannabinoid (CB2) agonist activity, thus lacking the psychomotor responses characteristic of Δ9-THC. HU-211 does exhibit the neuroprotective, antioxidant properties of other related compounds like cannabidiol. HU-211 also has anti-inflammatory properties derived through inhibition of NF-κB and the resulting decreases in cytokines such as TNFα and interleukin-6.
A synthetic endocannabinoid analog and potent 5-lipoxygenase inhibitor
Positive control for western blotting
A colorimetric FAAH substrate used for enzyme activity measurement
Decanoyl m-Nitroaniline (DemNA) is one of several nitroaniline fatty acid amides which can be used to measure fatty acid amide hydrolase (FAAH) activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its endogenous substrate anandamide (arachidonyl ethanolamide; AEA). It also will hydrolyze fatty acid amides with fewer carbons and fewer double bonds than arachidonate. Exposure of DemNA to FAAH activity results in the release of the yellow colorimetric dye m-nitroaniline (ε = 13,500 at 410 nm) This allows the fast and convenient measurement of FAAH activity using a 96 well plate spectrophotometer.
A colorimetric FAAH substrate for enzyme activity measurement
Arachidonoyl m-Nitroaniline (AmNA) is one of several nitroaniline fatty acid amides which can be used to measure fatty acid amide hydrolase (FAAH) activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate anandamide (arachidonyl ethanolamide; AEA). It also will hydrolyze fatty acid amides with fewer carbons and fewer double bonds than arachidonate (see also Decanoyl m-Nitroaniline; Catalog No. 90349). Exposure of AmNA to FAAH activity results in the release of the yellow colorimetric dye m-nitroaniline (ε = 13,500 at 410 nm). This offers the potential for fast and convenient measurements of FAAH activity using a 96 well plate spectrophotometer.
Internal standard for the quantification of CAY10429
CAY10429-d3 contains three deuterium atoms at the terminal methyl position. It is intended for use as an internal standard for the quantification of CAY10429 by GC- or LC-mass spectrometry.
Stable precursor of 4(5)-EpDPE, a CYP450 metabolite of DHA
A DHA congener of 14,15-EpETrE
EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as 14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) have been little studied relative to arachidonate epoxygenase metabolites. 16(17)-EpETE is the DHA homolog of 14(15)-EpETrE, derived via epoxidation of the 16,17-double bond of docosahexaenoic acid (DHA). The EDHF activity of 16(17)-EpDPE has not yet been determined. The epoxygenase metabolites of DHA have also been detected in a murine inflammation model.
A colorimetric FAAH substrate for enzyme activity measurement
Arachidonoyl p-nitroaniline (ApNA) is one of several nitroaniline fatty acid amides which can be used to measure fatty acid amide hydrolase (FAAH) activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate anandamide (AEA). It also will hydrolyze fatty acid amides with fewer carbons and fewer double bonds than arachidonate. (See also Decanoyl p-Nitroaniline - Catalog No. 90349).
15(S)-HETE ethanolamide is less potent than AEA at the CB1 receptor (Ki of 600 versus 90 nM). 15(S)-HETE ethanolamide also inhibits fatty acid amide hydrolase.
Novel dietary CNS dopamine enhancing lipid
Certain chronic neurologic disorders, such as Parkinson’s disease, are caused by an insufficiency of the neurotransmitter dopamine secondary to the degeneration of substantia nigra dopaminergic neurons. N-(α-Linolenoyl) tyrosine (NALT) is a simple α-amide conjugate between the ω-3 essential fatty acid α-linolenate and the amino acid tyrosine. α-Linolenate is an important precursor to docosahexaenoic acid (DHA), a prominent brain polyunsaturated fatty acid, while tyrosine is the metabolic precursor for neuronal dopamine synthesis. NALT was prepared as a method for enhancing central nervous system (CNS) dopamine content by facilitated transport of the tyrosine precursor across the blood-brain barrier. In experimental rat models of dopamine insufficiency, NALT increased CNS dopamine levels and exhibited an activity profile consistent with an anti-Parkinson’s therapeutic agent.
A potent anti-inflammatory lipid mediator
Resolvin D1 (RvD1) is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase. A 17(R)-epimer of RvD1 can also be generated in aspirin-treated samples. Both RvD1 and its 17(R) configuration reduce human polymorphonuclear leukocyte (PMNL) transendothelial migration, the earliest event in acute inflammation, with EC50 values of ~30 nM. RvD1 and its aspirin-triggered form also exhibit a dose-dependent reduction in leukocyte infiltration in a murine model of peritonitis with a maximal inhibition of ~35% at a 10-100 ng dose.
For immunochemical detection of PSD95
A potent inhibitor of monoacylglycerol lipase
N-Arachidonyl maleimide (NAM) is a potent, irreversible inhibitor of monoacylglycerol lipase (MGL) or MGL-like activity in rat cerebellar membranes, exhibiting an IC50 value of 140 nM. Inhibition of MGL by the sulfhydryl-reactive maleimide group of NAM suggests a critical cysteine residue is present in the substrate-binding site of the enzyme.
A highly purified protein for fatty acid research
A questioned inhibitor of monoacylglycerol lipase
URB754 is reported to be a potent, noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 of 200 nM for the recombinant rat brain enzyme. However, data from other labs indicates that it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 µM. It inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 of 32 µM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 of 3.8 µM. It does not inhibit cyclooxygenase-1 (COX-1) or COX-2 at concentrations up to 100 µM. Inhibition of 2-AG hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.
An AEA analog with similar biological activity
Arachidonoyl amide is an analog of anandamide (AEA) that lacks the hydroxyethyl moiety. It is hydrolyzed by FAAH more effectively than AEA but exhibits significantly weaker binding to the human CB1 receptor with a Ki of 9.6 µM. Arachidonoyl amide and AEA exhibit similar binding and translocation into cells via the AEA transporter. It inhibits [3H]-AEA uptake into human astrocytoma cells with an IC50 of 9 µM. Arachidonoyl amide also inhibits rat glial gap junction cell-cell communication by 90% at a concentration of 20 µM.
An endocannabinoid found in brain and retina
Docosahexaenoyl ethanolamide (DHEA) is the ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for arachidonoyl ethanolamide (AEA). A 9.5 fold increase of DHEA was observed in brain lipid extracts from piglets fed a diet supplemented with docosahexaenoic acid (DHA) compared to a control diet without DHA. DHEA binds to the rat brain CB1 receptor with a Ki of 324 nM, which is approximately 10-fold higher than the Ki for AEA. DHEA inhibits shaker-related voltage-gated potassium channels in brain slightly better than AEA, with an IC50 of 1.5 µM.
An irreversible COX-2 inhibitor
N-(3-hydroxyphenyl)-Arachidonoyl amide (3-HPA) is an analog of AM404 (N-(4-hydroxyphenyl)-arachidonoy amide), which is a selective inhibitor of carrier-mediated transport of arachidonoyl ethanolamide (AEA). 3-HPA is metabolized by both cyclooxygenase-1 (COX-1) and COX-2 and was found to selectively and irreversibly inhibit COX-2 with an IC50 value of 2 µM.
An internal standard for the quantification of arachidonoyl glycine
NAGly-d8 contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14, and 15 positions. It is intended for use as an internal standard for the quantification of NAGly by GC- or LC-mass spectrometry.
A naturally-occurring N-acyl dopamine
Structurally, N-palmitoyl dopamine (PALDA) is the amide of palmitic acid and dopamine and is therefore a “hybrid” analog which incorporates components of both the anandamide-like and dopamine neurotransmitter pathways. Unlike N-arachidonoyl dopamine (NADA) and N-oleoyl dopamine (ODA), PALDA is nearly inactive as a vanilloid receptor 1 (VR1) ligand and fails to elicit hyperalgesic or nocifensive responses in vivo. However, PALDA exhibits an “entourage” effect at concentrations of 0.1-10 µM by potentiating the VR1-mediated effects of NADA and anandamide.
An internal standard for the quantification of N-arachidonoyl dopamine
N-Arachidonoyl dopamine-d8 contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14, and 15 positions. It is intended for use as an internal standard for the quantification of N-arachidonoyl dopamine by GC- or LC-mass spectrometry.
A selective acidic PEAase inhibitor
N-Cyclohexanecarbonylpentadecylamine is a selective inhibitor of acidic palmitoyl ethanolamidase, inhibiting the enzyme with an IC50 of 4.5 µM, while failing to inhibit fatty acid amide even at 100 µM.
A FAAH substrate discovered during metabolite profiling
N-Docosanoyl taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of brain and spinal cord from wild-type and fatty acid amide hydrolase (FAAH) knockout mice. The levels of N-docosanoyl taurine were elevated ~12 fold in FAAH-/- mice compared to wild-type mice, indicating that FAAH utilizes N-docosanoyl taurine as a substrate. However, in vitro experiments with purified FAAH indicate that related N-fatty acyl taurines and ethanolamines of similar chain length are hydrolyzed 2,000-50,000 times more slowly by FAAH compared to oleoyl ethanolamide. N-acyl taurines bearing polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) family of calcium channels, including TRPV1 and TRPV4.
Designed for the convenient, precise quantification of Arachidonoyl Ethanolamide
Arachidonoyl ethanolamide (AEA) is the ethanolamine amide of arachidonic acid, first isolated from porcine brain. AEA is an endogenous cannabinoid neurotransmitter that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. AEA inhibits the specific binding of [3H]-HU-243 to synaptosomal membranes with a Ki value of 52 nM, compared to 46 nM for Δ9-THC.
A CB1 receptor ligand
Arachidonoyl-N-methyl amide is an analog of anandamide that binds to the human central cannabinoid (CB1) receptor with a Ki of 60 nM. It inhibits rat glial gap junction cell-cell communication 100% at a concentration of 50 µM.
An AEA analog with weak CB1 receptor affinity
Arachidonoyl-N,N-dimethyl amide is an analog of anandamide that exhibits weak or no binding to the human central cannabinoid (CB1) receptor (Ki >1 µM). It inhibits rat glial gap junction cell-cell communication 100% at a concentration of 50 µM.
A FAAH substrate discovered during metabolite profiling
N-lignoceroyl taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of brain and spinal cord from wild-type and fatty acid amide hydrolase (FAAH) knockout mice. The levels of N-lignoceroyl taurine were elevated 23-26 fold in FAAH-/- mice compared to wild-type mice, indicating that FAAH utilizes N-lignoceroyl taurine as a substrate. However, in vitro experiments with purified FAAH indicate N-lignoceroyl taurine is hydrolyzed 2,000 times more slowly by FAAH compared to oleoyl ethanolamide. N-acyl taurines bearing polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) family of calcium channels, including TRPV1 and TRPV4.
A FAAH substrate discovered during metabolite profiling
N-Nervonyl taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of brain and spinal cord from wild-type and fatty acid amide hydrolase (FAAH) knockout mice. The levels of N-nervonyl taurine were elevated ~25 fold in FAAH-/- mice compared to wild-type mice, indicating that FAAH utilizes N-nervonyl taurine as a substrate. However, in vitro experiments with purified FAAH indicate that related N-fatty acyl taurines and ethanolamines of similar chain length are hydrolyzed 2,000-50,000 times more slowly by FAAH compared to oleoyl ethanolamide. The biological function of the taurine fatty acids class of molecules, as well as their relevance to endocannabinoid signaling, remains to be determined. N-acyl taurines bearing polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) family of calcium channels, including TRPV1 and TRPV4.
Designed for the convenient, precise quantification of Prostaglandin D2-d4
PGD2-d4 contains four deuterium atoms at the 3, 3', 4, and 4' positions. It is intended for use as an internal standard for the quantification of PGD2 by GC- or LC-mass spectrometry.
An immunometric EIA for use with human L-PGDS
Cayman’s Prostaglandin D Synthase (human lipocalin-type) (L-PGDS) EIA Kit is an immunometric (i.e., sandwich) EIA. The standard curve ranges from 0-100 ng/ml, with a limit of detection of 6 ng/ml. Inter- and intra-assay CV’s of less than 15% may be achieved at most concentrations. L-PGDS is present in a variety of body fluids including cerebrospinal fluid, seminal fluid, and plasma. This assay has been validated using cerebrospinal fluid which contains approximately 12-30 µg/ml of L-PGDS.
Trimebutine is a spasmolytic with possible local anesthetic action used in gastrointestinal disorders.
2-cyano-3-(3,4-dihydrocy-5-nitrophenyl)-N,N-diethyl-2-propenamide-d10
Entacapone is a catechol-O-methyl transferase inhibitor for the treatment of Parkinson’s disease. When administered in conjunction with dopaminergic agents such as L-DOPA, entacapone increases the bioavailability of these compounds by facilitating their passage across the blood-brain barrier. It is a member of the class of nitrocatecholes.
Lercanidipine is a calcium channel blocker of the dihydropyridine class.
Trimebutine is a spasmolytic with possible local anesthetic action used in gastrointestinal disorders.
For immunochemical detection of CaMKII
For immunochemical detection of CaMKII
For immunochemical detection of PSD95
Capsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in order to obtain capsaicin of consistently high purity and reproducible quality. VR1 is a heat-activated calcium ion channel which functions as part of the normal nociceptive pain pathway. Capsaicin elicits a sensation of burning pain by activation of VR1 on small, non-myelinated polymodal C-type nociceptive nerve fibers. Chronic application of capsaicin leads to desensitization of these pain fibers and has been widely exploited in various non-prescription pain remedies.
An exceptionally potent FAAH inhibitor
CAY10402 is a potent FAAH inhibitor, exhibiting Ki values of 0.094 nM and 0.2 nM for the human and rat enzymes, respectively.
The COX-inactive enantiomer of Flurbiprofen (Ansaid)
(R)-Flurbiprofen is a member of the 2-aryl propionic acid group of nonsteroidal anti-inflammatory drugs (NSAIDs). Only a small amount (<5%) of (R)-enantiomer is converted to the (S)-enantiomer in rats and humans; therefore, the biological effects are specific to each enantiomer. Although inactive as an inhibitor of cyclooxygenase (COX), this enantiomer reduces inflammation through inhibition of NF-κB and AP-1 activation. (R)-Flurbiprofen has also been shown to suppress prostate tumor cells by inducing p75NTR protein expression. (R)-Flurbiprofen inhibits the enzyme γ-secretase thereby preventing the formation of the amyloid β peptide (Aβ42) from amyloid β precursor protein (APP). Before being dropped as a drug candidate, (R)-flurbiprofen advanced to Phase III clinical trials, the first drug candidate to advance to late stage trials for the treatment of mild Alzheimer’s disease.
An exceptionally potent FAAH inhibitor
CAY10401 is a selective, potent inhibitor of rat FAAH exhibiting a Ki value of 0.14 nM. CAY10401 is approximately 580 fold more potent than oleyl trifluoromethyl ketone when assayed under the same conditions.
Analog of arachidonoyl ethanolamide
A potent CB2 receptor agonist
GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively. When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.
A non-CB1/CB2 receptor agonist
CAY10429 (abnormal cannabidiol) is a synthetic regioisomer of cannabidiol that fails to elicit either CB1 or CB2 responsiveness and is without psychotropic activity. CAY10429 induces endothelium-dependent vasodilation via a CB1/CB2/NO-independent mechanism. At a dose of 20 µg/g in rats, CAY10429 showed hypotensive activity that could not be antagonized by cannabidiol or SR141716A. CAY10429 is therefore believed to activate a third type of cannabinoid receptor, provisionally called the non-CB1/CB2 endocannabinoid receptor. CAY10429 also acts via these receptors to regulate the migratory activity of murine BV-2 microglial cells, with an EC50 of 600 nM.
A selective antagonist of abnormal cannabidiol-mediated effects
O-1918 is a cannabidiol analog that acts as a selective antagonist of abnormal cannabidiol at the non-central cannabinoid/peripheral cannabinoid (non-CB1/CB2) endothelial receptor. It does not bind to CB1 or CB2 receptors at concentrations up to 30 µM and inhibits the vasorelaxant effects of abnormal cannabidiol in vitro and in whole animals. It also blocks the abnormal cannabidiol-induced activation of the phosphatidylinositol 3-kinase/Akt pathway in human umbilical vein endothelial cells.
A water soluble prodrug AEA analog
The phosphate ester of R-1 methanandamide, R-1MAP, has been tested as a water soluble prodrug analog of AEA. The activity of R-1MAP was essentially equivalent to that of AEA in the growth inhibition of C6 glioma cells. However, when tested for inhibition of AEA binding to isolated rat brain CB1 receptors, arachidonoyl ethanolamide phosphate (AEA-P) is about 5-fold less potent as an agonist with a Ki of about 200 nM. The phosphate esters of AEA and its analogs are also structural variants of lysophosphatidic acid (LPA). However, the effects of R-1MAP on the various LPA receptors have not been tested.
A potent CB1 receptor antagonist
NESS 0327 is an extremely potent cannabinoid (CB) receptor antagonist with high selectivity for the CB1 receptor compared to the CB2 receptor with Ki values of 0.35 pM and 21 nM, respectively. It is a much more potent antagonist and more selective for the CB1 receptor compared to SR 141716A (rimonabant). At nM concentrations NESS 0327 competitively inhibits the binding of the synthetic CB agonist WIN 55,212-2 in isolated rat cerebella membranes and murine vas deferens. Unlike SR 141716A, NESS 0327 at higher doses does not act as a CB1 receptor inverse agonist and does not produce any physiological effects of its own.
An internal standard for the quantification of linoleoyl ethanolamide by GC- or LC-MS
A colorimetric method for screening MGL inhibitors
Cayman’s Monoacylglycerol Lipase (MAGL) Inhibitor Screening Assay provides a convenient method for screening human MAGL inhibitors. MAGL hydrolyzes 4-nitrophenylacetate resulting in a yellow product, 4-nitrophenol, with an absorbance of 405-412 nm.
An internal standard for the quantification of OEA by GC- or LC-MS
An internal standard for the quantification of PEA
For D and E series prostaglandin analog screening
This screening plate contains wide range prostaglandins in the “D and E-series” configuration (9-keto, 11-keto, 9-hydroxy, and 11-hydroxy prostaglandins).
For A and J series prostaglandin analog screening
This screening plate contains wide range prostaglandins in the “A and J-series”.
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