For the quantification of 11-dehydro TXB₂ in urine and other sample matrices

Limit of detection: 80% B/B₀: 34 pg/ml · Sensitivity: 50% B/B₀: 120 pg/ml · Thromboxane A₂ (TXA₂), produced from arachidonic acid, causes irreversible platelet aggregation, vascular, and bronchial smooth muscle contraction. TXA₂ is rapidly hydrolyzed non-enzymatically to form TXB₂. However, most of the TXB₂ measured in the plasma or urine of healthy individuals is due to ex vivo platelet activation or intra-renal production, and normal concentrations of circulating TXB₂ are extremely low (1-2 pg/ml) and highly transient (t1/2 = 5-7 minutes). 11-dehydro TXB₂ is a metabolite of TXB₂ (not formed by platelets or the kidney) with a circulating half-life (t1/2) of 45 minutes. Its measurement in plasma or urine will give a time-integrated indication of TXA₂ production and is recommended to estimate TXA₂ levels to circumvent measurement complications associated with TXB₂. Cayman’s 11-dehydro TXB₂ EIA Kit is a competitive assay that can be used for quantification of 11-dehydro TXB₂ in urine and other sample matrices. Normal plasma levels of 11-dehydro TXB₂ (1-2 pg/ml) are below the detection limit of this assay (16 pg/ml), so plasma samples must be purified and concentrated prior to analysis. Urine samples should be diluted appropriately before assaying. There is evidence suggesting that 11-dehydro TXB₂ can be formed non-enzymatically following platelet activation, so it is important to process plasma samples quickly to prevent artifactual formation of 11-dehydro TXB₂. The EIA typically displays an IC₅₀ (50% B/B₀) value of 120 pg/ml and a detection limit (80% B/B₀) of approximately 34 pg/ml.

A side-chain substituted oxysterol

25-hydroxy Cholesterol is a side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of sterol regulatory element binding proteins (SREBPs) to suppress endogenous cholesterol synthesis in various cell types. It has been implicated in a variety of metabolic events including cholesterol homeostasis and atherosclerosis as well as antitumor activities as it has been shown to induce apoptosis through down-regulation of Bcl-2 expression and activation of caspases. Immunomodulating capabilities have also been observed as the oxysterol can act as a LXR-RXR ligand coupling cholesterol synthesis to T cell proliferation, can reduce (EC₅₀ ~ 65 nM) IgA production by B cells in response to IL-2, and can suppress differentiation of monocytes into macrophages.

Isomer of 4-FA

2-Fluoroamphetamine (2-FA) (hydrochloride) is a structural isomer of 4-FA, having the fluorine at the 2, rather than the 4, position. The physiological and toxicological properties of 2-FA are not known. This product is intended for research and forensic applications.

Isomer of 4-FA

3-Fluoroamphetamine (hydrochloride) is a structural isomer of 4-FA, having the fluorine at the 3, rather than the 4, position. The physiological and toxicological properties of 3-FA are not known. This product is intended for research and forensic applications.

An internal standard for the quantification of DMABA NHS ester

DMABA-d₆ NHS ester is intended for use as an internal standard for the quantification of DMABA NHS ester by GC- or LC-mass spectrometry.

Highly potent 5-HT2A receptor agonist

25I-NMBOMe, a derivative of the phenethylamine hallucinogen 2C-I, is a highly potent agonist for the human 5-HT2A receptor with a K_i value of 0.044 nM, making it 16-fold more potent than 2C-I. A radiolabelled form of 25I-NBOMe has been used for mapping the distribution of 5-HT2A receptors in the brain.

Positional isomer of methedrone

2-Methoxymethcathinone (hydrochloride) is a positional isomer of methedrone, having the methoxy group at the 2 rather than the 4 position. It is also the β-keto derivative of 2-methoxymethamphetamine, a β-adrenergic receptor agonist used as a bronchodilator. The properties of 2-methoxymethcathinone have been poorly studied. This product is intended for forensic and research applications.

A potential designer drug

3-Methylethcathinone (hydrochloride) is a substituted cathinone with potential for abuse. Its biological properties have not been elucidated. This product is intended for forensic and research applications.

A UV blocker with estrogenic effects

4-Methylbenzylidene camphor is an ultraviolet light blocker used in cosmetics and sunscreen preparations that also has estrogenic activities. It has estrogenic activity in fish and in mammals, binding competitively to estrogen receptors and stimulating transactivation. In addition to reducing receptor sensitivity to estradiol, 4-MBC directs dose-dependent changes in the expression of estrogen receptor subtypes, progesterone receptor, and androgen receptor. This results in changes in reproductive organ and brain development in both males and females. When applied topically, it is absorbed systemically and can be detected in urine.

A synthetic cannabinoid agonist

AM1248 is an adamantoylindole derivative with an N-methylpiperidin-2-ylmethyl substitution at the indole 1-position. It reportedly acts as a moderately potent agonist for both the central CB₁ and peripheral CB₂ cannabinoid receptors (Kis = 11.9 and 4.8 nM, respectively). A related compound, 1-pentyl-3-(1-adamantoyl)indole, along with another synthetic cannabinoid, AM679, was identified as having been sold as a cannabinoid herbal blend known as “smart products” in Hungary in 2011.

A pan-HDAC inhibitor

SB 939 is an HDAC inhibitor that displays an IC₅₀ value of 77 nM in an in vitro HDAC1 activity assay and prevents proliferation of ovarian (A2780), colon (COLO 205 and HCT-116), and prostate cancer (PC-3) cell lines at IC₅₀ values of 0.48, 0.56, 0.48, and 0.34 μM, respectively. SB 939 is a pan-HDAC inhibitor binding all HDAC isozymes with similar affinity (Kis = 16-28 nM) with the exception of HDAC6 and 7 (Kis = 247 and 104 nM, respectively). SB 939 demonstrates good bioavailability in vivo and significantly inhibits tumor growth in various xenograft mouse models at doses ranging from 25-100 mg/kg. It is being evaluated in phase I and phase II clinical trials in both hematological and solid tumor patients.

A potential designer drug

3-Fluoroethcathinone (hydrochloride) is a fluorine-substituted synthetic cathinone that has potential for abuse. The physiological and toxicological properties of this compound are unknown. This product is intended for forensic and research applications.

A potential impurity of 4-methylmethcathinone

3-Methylmethcathinone (hydrochloride) is a potential major impurity in preparations of 4-MMC. As an isomer of 4-MMC, it is likely to have psychoactive properties and may itself be marketed as a designer drug. The physiological and toxicological properties of this compound have not been determined. This product is intended for forensic and research applications.

A detection marker for illicit opiates

Meconin, a noscapine metabolite, is a urinary detection marker for illicit opiate misuse. This product is intended for use as a forensic standard.

Peptide sequence: N-terminal acetylated-PGP ·

A major urinary metabolite of PGD₂

PGDM is a major urinary metabolite of PGD₂ with a unique lower sidechain that readily undergoes reversible cyclization. It is used as a biomarker to assess endogenous production of PGD₂.

An internal standard for the quantification of PGDM

PGDM-d₄ contains four deuterium atoms at the 18, 18', 19 and 19' positions. It is intended for use as an internal standard for the quantification of PGDM by GC- or LC-mass spectrometry.

Peptide sequence: PGP ·

The synthetic CB HPLC mixture V (AM series) contains a selection of the most common AM CB receptor agonists. Several of these synthetic CBs have been identified in commercial herbal blends which are being misused as designer drugs. The synthetic CB HPLC mixture is intended to be used for the development of analytical screening methods for the identification of these compounds in such products. Contents: AM630, AM694, AM1220, AM1241, AM2201, and AM2233.

An anti-inflammatory lipid produced by macrophages

7(R)-Maresin 1 (7(R)-MaR1) is a 7, 14-dihydroxy DHA formed from 14S-hydroperoxy DHA supplied exogenously to resident peritoneal mouse macrophages activated with zymosan A. It potently reduces infiltration of neutrophils into the murine peritoneum in zymosan A-induced peritonitis when given intravenously (0.2 ng) and significantly increases phagocytosis of FITC-labeled zymosan A by isolated murine macrophages (0.1-100 nM).

Source: recombinant N-terminal GST-tagged protein expressed in E. coli · M_r: 61.2 kDa ·

A mycotoxin

Alternariol is a mycotoxin, a toxic secondary fungal metabolite, produced by Alternaria molds. It is cytotoxic, fetotoxic, teratogenic, mutagenic, and genotoxic. It induces cytochrome P450 1A1 expression and apoptosis in mouse hepatoma cells (20-40 μM). Alternariol, whose synthesis is inhibited by light, naturally occurs on fruits, vegetables, and cereals, such as apples, tomatoes, and wheat.

Inhibitor of α- and β-glucosidases

Castanospermine is an inhibitor of both α- and β-glucosidases, inhibiting lysosomal and neutral α-glucosidases with K_i values of 0.1 and 10 μM, respectively, and lysosomal and cytosolic β-glucosidases with K_i values of 7 and 40 μM, respectively. It is effective both in vitro and in vivo. Through its effects on glucosidases, castanospermine blocks N-linked glycosylation during post-translational modification of proteins, affecting protein trafficking and cell functions that are dependent on glycosylation, including angiogenesis. Castanospermine also interferes with viral replication and infection that is dependent on glucosidase activity.

Potent inhibitor of PKC and BclXL

Chelerythrine chloride is a potent, cell permeable inhibitor of protein kinase C (IC₅₀ = 660 nM) that does not inhibit tyrosine protein kinases, cAMP-dependent protein kinase, or calcium/calmodulin-dependent protein kinase. Chelerythrine also inhibits BclXL function (IC₅₀ = 1.5 μM) by displacing Bax binding, inducing apoptosis in several cancer cell lines. Chelerythrine can also have PKC-independent effects, activate p38 MAP kinase and JUNK signaling pathways, and induce apoptosis in cancer cells both in vitro and in vivo.

Positional isomer of JWH 210

JWH 210 6-ethylnaphthyl isomer is a positional isomer of JWH 210, having the ethyl side chain at the 6 position rather than at the 4 position of the naphthyl group. The biological activities of this isomer have not been determined. This product is intended for forensic purposes.