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Request The Product List ofProstaglandin Receptor Prostaglandin Receptor

Prostaglandin receptor, a sub-family of cell surface seven-transmembrane receptors, are the G-protein-coupled receptors. There are currently ten known prostaglandin receptors on various cell types. Prostaglandins bind to a subfamily of cell surface seven-transmembrane receptors, G-protein-coupled receptors. These receptors are named: DP1-2-DP1, DP2 receptors, EP1-4-EP1, EP2, EP3, EP4 receptors, FP-FP, IP1-2-IP1, IP2 receptors, TP-TP receptor. The prostaglandins are a group of hormone-like lipid compounds that are derived enzymatically from fatty acids and have important functions in the animalbody. There are currently ten known prostaglandin receptors on various cell types.

Cat. No. Product Name CAS No. Information
H9263

BAY 73-1449

693790-96-4

BAY 73-1449 is a selective antagonist of prostacyclin IP receptor, with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG;BAY 73-1449 can be used in the research of lowering blood pressure.

H8879

Ebopiprant

2005486-31-5

Ebopiprant(OBE022)is a potent, highly selective, orally active antagonist of the contractile PGF2α prostaglandin receptor with Kb of 5.9 nM, shows no activity for other human PG receptors subtypes; inhibits spontaneous, oxytocin- and PGF2α-induced human myometrial contractions alone and is more effective in combination with atosiban or nifedipine; reduces spontaneous contractions in near-term pregnant rat, OBE022 delayed RU486-induced parturition and exerted synergistic effects in combination with nifedipine; exhibits potent tocolytic effects on human tissues ex vivo and animal models in vivo without causing the adverse fetal side effects.

H8756

Treprostinil palmitil

1706528-83-7

Treprostinil palmitil is a prodrug of Treprostine (TRE)

H8611

KAG-308

1215192-68-9

KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.

H3850

U-46619

56985-40-1

U-46619 is a potent and stable thromboxane A2 (TP) receptor agonist with EC50 of 35 nM; activates ERK-1 and ERK-2 in HEK 293 cells expressing TPα and TPβ receptors, and potently stimulates TP receptor-mediated, but not other prostaglandin receptor-mediated responses in vitro.

H3849

TG8-69

2281765-16-8

TG8-69 is a peripherally restricted, highly potent, selective, aqueous-soluble EP2 antagonist with Kb of 48.5 nM; inhibits PGE2 induced EP2 receptor activation in a concentration-dependent manner in cAMP mediated TR-FRET based functional EP2 assay, inhibits the binding of radiolabeled H3-PGE2 to EP2 receptors with Ki of 135 nM; displays >1000-fold selectivity ober other Gαs-coupled prostanoid receptors, DP1, EP4, and IP; demonstrates anti-inflammatory properties.

H3848

TG6-10-1

1415716-58-3

A potent and selective antagonist of prostaglandin E2 receptor subtype EP2 with Kb of 17.8 nM; displays >300-fold selectivity over EP3, EP4, and IP receptors, 100-fold selectivity over EP1, 25-fold selectivity over FP and TP, and 10-fold selectivity over DP1 receptors; completely recapitulates the effects of conditional ablation of COX-2 from principal forebrain neurons, accelerates recovery from weight loss, reduces brain inflammation, prevention of blood-brain barrier opening, and neuroprotection in the hippocampus, without modifying seizures acutely in the mouse pilocarpine model of SE.

H3847

TG4-155

1164462-05-8

TG4-155 is a potent and selective prostaglandin EP2 receptor antagonist with Kb of 2.4 nM; displays 4,730-fold selectivity over EP4, >500-fold selectivity over human BLT1, EP1, EP3, and FP receptors, and 7-fold selectivity against human DP1 receptor; displays robust inhibition of PGE2-induced cAMP accumulation in C6G cells stably expressing mouse EP2 receptor; significantly reduces SE-induced neurodegeneration in mice.

H3846

Terutroban

165538-40-9

Terutroban (S-18886) is a potent, selective antagonist of the thromboxane receptor (Prostanoid TP receptor) that blocks thromboxane induced platelet aggregation and vasoconstriction;

H3845

TASP0376377

1233246-60-0

TASP0376377 is a potent, selective prostaglandin D2 receptor (CRTH2) antagonist with binding IC50 of 19 nM; shows excellent functional antagonist activity in chemotaxis assay with IC50 of 23 nM, displays sufficient selectivity for binding to CRTH2 over the DP1 prostanoid receptor (IC50>1 yM), COX-1 and COX-2 enzymes (IC50>10 uM).

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