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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