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Tools to Study Eicosanoid GPCR Signaling

Article from 2021-02-22

Lipids, as an entire class of biomolecules, cover a broad range of species. Some serve primarily as structural components of cell membranes or as energy storage depots, while others are active signaling molecules that are generated by cell activation events. Many signaling lipids bind to G protein-coupled receptors (GPCRs) to transmit signals that affect numerous biological activities. This includes platelet activation, vasoconstriction/dilation, leukocyte chemoattraction, smooth muscle constriction, and many others. The major eicosanoids—prostaglandins, thromboxanes, and leukotrienes—mediate biological effects by binding with specific G_s-, G_i-, or G_q-coupled receptors. Several GPCRs have been deorphanized by the discovery of eicosanoids activating their signaling. We’ve created a wall poster to delineate what is currently known about these distinct pathways.

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Cayman offers an extensive library of agonists, antagonists, assays, and antibodies to study the function of these receptors. Use the tables below to navigate to research products associated with each eicosanoid GPCR.

G_s These receptors couple to G_s to activate adenylyl cyclase, which stimulates the cyclic AMP-dependent pathway.	DP₁ actions	Agonists	Antagonists	Assays & Antibody
	· Relaxes smooth muscle · Inhibits platelet aggregation · Suppresses leukocyte function · Mediates nasal congestion	PGD₂ 15(S)-15-methyl PGD₂ BW 245C BW 246C ZK118182 isopropyl ester	AH 6809 Asapiprant BW A868C MK-0524 S-5751	DP₁ Receptor Polyclonal Antibody PGD₂ ELISA Kit PGD₂ Express ELISA Kit PGD₂-MOX ELISA Kit PGD₂-MOX Express ELISA Kit 11β-PGF_2α ELISA Kit tetranor-PGDM ELISA Kit
	EP₂ actions	Agonists	Antagonists	Assays & Antibodies
	· Relaxes smooth muscle, dilation · Mediates bone formation · Suppresses leukocyte function · Mediates spinal inflammatory hyperalgesia · Inhibits sleep · Promotes ovarian follicle growth · Stimulates renin release · Offers neuroprotection	PGE₂ 11-deoxy PGE₁ 11-deoxy-16,16-dimethyl PGE₂ 19(R)-hydroxy PGE₂ Butaprost Butaprost (free acid) CP 544,326 Misoprostol Misoprostol (free acid)	AH 6809 PF-04418948 TG4-155 TG6-10-1 TG6-129 TG11-77	EP₂ Receptor Polyclonal Antibody EP₂ Receptor Polyclonal PE Antibody EP₂ Receptor (rat) Reporter Assay Kit EP₂ Receptor (human) Reporter Assay Kit PGE₂ ELISA Kit - Monoclonal PGE₂ Express ELISA Kit PGE Metabolite ELISA Kit
	EP₄ actions	Agonists	Antagonists	Assays & Antibodies
	· Mediates renal vasodilation · Mediates bone production · Suppresses leukocyte function · Promotes sleep · Promotes ovarian follicle growth · Stimulates renin release; salt and water excretion · Regulates gastric acid and duodenal HCO₃^- secretion	PGE₂ CAY10580 CAY10598 CAY10684 KMN-80 L-902,688 Misoprostol Misoprostol (free acid) Rivenprost	AAT-008 AH 23848 ASP7657 BGC 20-1531 CAY10580 CJ-023423 CJ-42794 E7046 EP₄ Receptor Antagonist 1 GW 627368X L-161,982 MF498 ONO-AE3-208	EP₄ Receptor (N-Term) Polyclonal Antiserum EP₄ Receptor (C-Term) Polyclonal Antibody EP₄ Receptor (C-Term) Polyclonal PE Antibody Anti-EP₄ Receptor (C-Term):SureLight^® APC EP₄ Receptor (rat) Activation Assay Kit (cAMP) EP₄ Receptor (rat) Reporter Assay Kit EP₄ Receptor (human) Reporter Assay Kit PGE₂ ELISA Kit - Monoclonal PGE₂ Express ELISA Kit PGE Metabolite ELISA Kit
	IP actions	Agonists	Antagonists	Assays & Antibodies
	· Relaxes pulmonary arterial, bronchial smooth muscle · Inhibits platelet aggregation · Suppresses cardiomyocyte hypertrophy Secondary coupling to G_i	PGI₂ PGI₃ AFP 07 Beraprost Carbaprostacyclin 13,14-dehydro-15-cyclohexyl Carbaprostacyclin Cicaprost Ciprostene Iloprost MRE-269 NS-304 Ralinepag Taprostene Treprostinil	CAY10441 CAY10449	IP Receptor (mouse) Polyclonal Antibody IP Receptor (human) Polyclonal Antibody 6-keto PGF_1α ELISA Kit PGI Metabolite ELISA Kit

G_i These receptors couple to G_i to inhibit cyclic AMP production and to mobilize intracellular calcium.	DP₂ (CRTH2) actions	Agonists	Antagonists	Assays & Antibodies
	Activates eosinophils; mediates chemotaxis and degranulation · Stimulates inflammatory cytokine production · Mediates lymphocyte and basophil infiltration	PGD₂ 15(R)-PGD₂ 15(R)-15-methyl PGD₂ 15-deoxy-Δ^12,14-PGD₂ 13,14-dihydro-15-keto PGD₂ 17-phenyl trinor PGD₂ Δ¹²-PGJ₂ 15-deoxy-Δ^12,14-PGJ₂ 11-keto Fluprostenol Indomethacin	AZD 1981 BAY u3405 BI-671800 CAY10471 CAY10595 CAY10597 Fevipiprant LAS191859 OC000459 Setipiprant	CRTH2/DP₂ Receptor (N-Term) Polyclonal Antibody CRTH2/DP₂ Receptor (C-Term) Polyclonal Antibody PGD₂ ELISA Kit PGD₂ Express ELISA Kit PGD₂-MOX ELISA Kit PGD₂-MOX Express ELISA Kit 11β-PGF_2α ELISA Kit tetranor-PGDM ELISA Kit
	EP₃actions	Agonists	Antagonists	Assays & Antibodies
	· Contracts smooth muscle; constricts vessels, venules, and airways · Inhibits gastric acid and duodenal HCO₃^- secretion · Mediates mechanical/thermal hyperalgesia · Inhibits lipolysis Secondary coupling to G_q	PGE₂ 11-deoxy-16,16-dimethyl PGE₂ 17-phenyl trinor PGE₂ 19(R)-hydroxy PGE ₁ Misoprostol Misoprostol (free acid) Sulprostone	AH 6809 L-798,106 L-826,266	EP₃ Receptor Polyclonal Antibody PGE₂ ELISA Kit - Monoclonal PGE₂ Express ELISA Kit PGE Metabolite ELISA Kit
	BLT₁ actions	Agonists	Antagonists	Assays & Antibodies
	· Mediates leukocyte aggregation, chemotaxis, and chemokinesis · Roles in atherosclerosis, asthma, and inflammation Secondary coupling to G_q	LTB₄ 20-trifluoro LTB₄ LTB₄-3-aminopropylamide LTB₃	LTB₄ Ethanolamide LTB₄ dimethyl amide 20-hydroxy LTB ₄ 14,15-dehydro LTB₄ LY223982 LY293111 γ-Linolenic Acid ethyl ester Resolvin E1 U-75302	BLT₁ Receptor Polyclonal Antibody BLT₁ Receptor Polyclonal Antiserum BLT₁ Receptor Monoclonal Antibody (Clone 7B1) LTB₄ ELISA Kit LTB₄ Express ELISA Kit
	BLT₂ actions	Agonists	Antagonist	Assays & Antibody
	· Actions redundant to BLT₁ · May play a role in itch-induced scratching · Activated by HETEs Secondary coupling to G_q	LTB₄ CAY10583 12(S)-HETE 12(S)-HHTrE 12-OxoETE	LY255283	BLT₂ Receptor Polyclonal Antibody LTB₄ ELISA Kit LTB₄ Express ELISA Kit
	OXER1 actions	Agonists	Antagonist	Antibody
	· Stimulates chemotaxis and adherence	5-OxoETE 5-OxoETE methyl ester 5(S)-HETE	Gue1654	5-OxoETE Receptor Polyclonal Antibody
	ALX/FPR2 actions	Agonists	Antagonists	Assay & Antibody
	Stimulates chemotaxis and adherence	LXA₄ 15(R)-LXA₄ Resolvin D1	Unknown	FPR2 (C-Term) Polyclonal Antibody LXA₄ ELISA Kit
	12-HETER1 (GPR31) actions	Agonist	Antagonists	Antibodies
	Stimulates chemotaxis, adherence, and angiogenic responses	12(S)-HETE	Unknown	GPR31 (N-Term) Polyclonal Antibody GPR31 (C-Term) Polyclonal Antibody
	CMKLR1 (ERV1) actions	Agonist	Antagonists	Antibody
	Activates innate and adaptive immune cells	Resolvin E1	Unknown	CMKLR1 Polyclonal Antibody
	CysLT_E actions	Agonist	Antagonist	Assay
	Contracts smooth muscle · Enhances airway responsiveness · Mediates vascular leak (edema) · Mediates eosinophil chemoattraction	LTE₄	Montelukast	LTE₄ ELISA Kit

G_q These receptors couple to G_q to activate phospholipase C, which sets off a signaling cascade that ultimately releases stored calcium and activates protein kinase C.	EP₁ actions	Agonists	Antagonists	Assays & Antibody
	· Constricts airways; mediates renal vasoconstriction · Mediates hyperalgesia, allodynia, and mechanical/thermal analgesia · Regulates circadian clock · Protects gastric mucosa · Mediates thermoregulation · Inhibits sleep Secondary coupling to G_i	PGE₂ 17-phenyl trinor PGE₂ 19(R)-hydroxy PGE₁ Iloprost	AH 6809 GW 848687X ONO-8130 ONO-8711 SC-19220 SC-51089 SC-51322	EP₁ Receptor Polyclonal Antibody PGE₂ ELISA Kit - Monoclonal PGE₂ Express ELISA Kit PGE Metabolite ELISA Kit
	FP actions	Agonists	Antagonists	Assays & Antibody
	Mediates luteolysis, muscle contraction Decreases intraocular pressure · Inhibits prolactin receptor expression in corpus luteum Secondary coupling to G_s	PGF_2α 20-ethyl PGF _2α CAY10509 CAY10510 (+)-Cloprostenol (±)-Cloprostenol (sodium salt) (+)-Cloprostenol (sodium salt) Fluprostenol Fluprostenol isopropyl ester Latanoprost Latanoprost (free acid) Latanoprostene Bunod 17-phenyl trinor PGF_2α 17-phenyl trinor PGF_2α ethyl amide 15(S)-15 methyl PGF_2α 16,16-dimethyl PGF_2α 16-phenoxy tetranor PGF_2α Tafluprost Tafluprost (free acid) Unoprostone	AL 8810 AL 8810 isopropyl ester PGF_2α dimethyl amide PGF_2α dimethyl amine	FP Receptor Polyclonal Antibody PGF Receptor Reporter Assay Kit PGF_2α ELISA Kit 13,14-dihydro-15-keto PGF_2α ELISA Kit 17-phenyl trinor PGF_2α ELISA Kit Latanoprost ELISA Kit Fluprostenol ELISA Kit
	TP actions	Agonists	Antagonists	Assays & Antibodies
	· Aggregates platelet · Mediates smooth muscle contraction, broncho- and vasoconstriction · Mediates cellular immune responses	Carbocyclic TXA₂ I-BOP U-44069 U-46619 U-51605	AH 23848 BAY u3405 BM 567 CAY10535 GW 627368X ICI 192605 I-SAP L-655,240 Picotamide Pinane TXA₂ Seratrodast S18886 SQ 29,548	TP Receptor (mouse) Polyclonal Antibody TP Receptor (human) Polyclonal Antibody TP Receptor (human) Polyclonal FITC Antibody TXB₂ ELISA Kit TXB₂ Express ELISA Kit - Monoclonal 11-dehydro TXB₂ ELISA Kit - Monoclonal
	GPR75 actions	Agonists	Antagonist	Assays & Antibodies
	· Mediates vasoconstriction · Interferes with insulin signaling · Drives obesity	20-HETE CCL5/RANTES	AAA
	CysLT₁ actions	Agonists	Antagonists	Assays & Antibodies
	Roles in asthma and allergic rhinitis · Mediates vaso- and bronchoconstriction · Mediates airway hyper-responsiveness · Controls hematopoietic cell trafficking · Regulates mast cell proliferation	LTC₄ LTD₄ LTE₄ 11-trans LTC₄ N-methyl LTC₄	BAY u9773 LY171883 MK-571 MK-571 (sodium salt) Montelukast Pranlukast Quininib REV 5901 Zafirlukast	CysLT₁ Receptor Polyclonal Antibody CysLT₁ Receptor Polyclonal FITC Antibody CysLT ELISA Kit CysLT Express ELISA Kit LTC₄ ELISA Kit LTE₄ ELISA Kit
	CysLT₂ actions	Agonists	Antagonists	Assays & Antibodies
	Role unclear, may cause increased vascular permeability · Potentially influences brain and cardiac function · May limit membrane expression and action of CysLT₁	LTC₄ LTD₄ LTE₄ 11-trans LTC₄ N-methyl LTC₄	BayCysLT₂ BAY u9773 HAMI3379 Quininib	CysLT₂ Receptor (N-Term) Polyclonal Antibody CysLT₂ Receptor (C-Term) Polyclonal Antibody CysLT ELISA Kit CysLT Express ELISA Kit LTC₄ ELISA Kit LTE₄ ELISA Kit

The Prostaglandin Screening ELISA Kit was developed for screening applications in which the relative amount of prostaglandin production for a large number of cell culture samples must be determined. The antiserum used in this assay exhibits high cross reactivity for most prostaglandins (e.g., PGE_1α, PGE_2α, PGF_1α, PGF_2α, PGF_3α), which allows for the quantification of all the prostaglandins in a given sample within a single assay. A full specificity profile can be viewed in the kit booklet (PDF).

Additionally, the Prostaglandin Screening Libraries and Bio-Active Lipid Screening Libraries offer a collection of Cayman's extensive, highly purified prostaglandin compounds conveniently packaged in a ready-to-use format in a 96-well Matrix tube rack as stock solutions in DMSO. These libraries are a cost-effective means to obtaining compound diversity and are amenable to high-throughput screening.

Explore more products to study the Cyclooxygenase, Cytochrome P450, and Lipoxygenase pathways available from Cayman

Cayman's scientists are lipid experts. If you need help with a custom synthesis, sample analysis, compound screening, or assay development, our scientists are here to help. Contact us to request a quote.

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