Prostaglandin Receptor

OBE022 (OBE022) is an oral and selective prostaglandin F2α (PGF2α) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively.

Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.

Etersalate (Eterylate) inhibits platelet function and decreases thromboxane A2 (TXA2) levels.

Terbogrel (BIBV 308SE) is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.

Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.

KF 13218 is a potent, selective and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.

p-Hydroxycinnamic acid (NSC 59260), a common dietary phenol, could inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.

LCB-2853 is an antagonist of thromboxane A2 (TXA2) receptor, with antiplatelet and antithrombotic activities.

MRE-269 (ACT-333679) is an active metabolite of selexipag, and acts as a selective IP receptor agonist.

CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM).

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.

MK-2894 sodium salt is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM).

MK-7246 S enantiomer is the less active enantiomer of MK-7246.

A potent, selective DP 2 antagonist

Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist.

Travoprost is a synthetic ester prodrug of a prostaglandin F2α analogue that inhibits I Kir6.2/Sur2a ion channel with an IC 50 value of 3μM.

Furprofen is an non-steroidal anti-inflammatory drug (NSAID) with analgesic properties.

Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist.

Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production.

NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca2+] mobilization following stimulation of cells with the alternative TP agonist U46609.

Beraprost sodium, a prostacyclin analog, is a stable and orally active prodrug of PGI2.

Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor.

Saikogenin D is isolated from?Bupleurum chinense, has anti-inflammatory effects.

Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726.