RO3244794

An IP receptor antagonist (Ki = 20 nM in isolated human platelets), selective for the IP receptor over a panel of 50 receptors at 10 µM but does bind to EP3, EP4, and TP receptors and the adenosine A3 receptor (Kis = 4,169, 1,820, 8,128, and 4,786 nM, respectively), inhibits carbaprostacyclin-induced cAMP accumulation in CHO-K1 cells expressing the human IP receptor (IC50 = 316 nM), prevents treprostinil-induced relaxation in U-46619-precontracted isolated rat pulmonary arteries at 1 µM, inhibits PGI2- or 12-HETrE-induced aggregation of isolated human platelet-rich plasma at 250 nM, decreases acetic-acid induced writhing and carrageenan-induced mechanical hyperalgesia and edema in rats, decreases the difference in weight distribution between the osteoarthritic and control hind paws in a rat model of sodium monoiodoacetate-induced osteoarthritis at 10 mg/kg. SMILES: O=C([C@H](NC(OCC1=CC2=CC(C3=CC=C(C=C3)F)=CC=C2O1)=O)CC4=CC=C(C=C4)F)O. InChi Code: InChI=1S/C25H19F2NO5/c26-19-6-1-15(2-7-19)11-22(24(29)30)28-25(31)32-14-21-13-18-12-17(5-10-23(18)33-21)16-3-8-20(27)9-4-16/h1-10,12-13,22H,11,14H2,(H,28,31)(H,29,30)/t22-/m1/s1. InChi Key: IDONYPMIPXYFLY-JOCHJYFZSA-N