Prostaglandin Receptor

AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.

KW-8232 free base, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.

Treprostinil (LRX-15) (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.

Asapiprant (S-555739) is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.

AM211 (AM211 free acid) is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.

Treprostinil (UT-15) sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.

An antagonist of CRTH 2 /DP 2

L 888607 is a potent, selective, stable and orally active CRTH2 agonist.

Quinotolast sodium (FR71021) in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.

AMG-009 is a potent antagonist of prostaglandin D2, with IC50 of 3 nM and 12 nM for CRTH2 and DP receptors, respectively.

RS-601 is a novel leukotriene D4 (LTD4)/thromboxane A2 (TxA2) dual receptor antagonist, with antiasthmatic activities.

MK-8318 is a potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.

Benorylate (Salipran) is the esterification product of paracetamol and acetylsalicylic acid.

CRTh2 antagonist 1 is a CRTh2 antagonist with an IC50 of 89 nM.

Taprenepag isopropyl (PF-04217329) is a highly selective EP2 receptor agonist.

MK-447 is a free radical scavenger, also a nonsteroidal antiinflammatory agent, and enhances the formation of the endoperoxide, PGH2, and other prostaglandins.

AGN 210676 (Simenepag) is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 nM.

L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.

YM158 free base (YM-57158) is a potent and selective LTD4 and TXA2 receptor antagonist with pA2 values of about 8.87 and 8.81, respectively.

CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.

KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.

CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.

CRTH2-IN-1 (Ramatroban analog) (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 6 nM in a human DP2 binding assay.

Bunaprolast (U66858) (U66858) is a potent inhibitor of LTB4 production in human whole blood.