Vorapaxar

A potent, selective and orally active thrombin receptor PAR-1 antagonist with Ki of 8.1 nM; displays no activity against e PAR-2, PAR-3 and PAR-4, and no CYP450 enzyme inhibition potential; inhibits thrombin (10 nM) induced human platelet aggregation with IC50 of 47 nM; inhibits haTRAP-induced platelet aggregation in vivo.Thrombosis Approved (In Vitro) :Vorapaxar (SCH 530348) shows potent inhibition of thrombin-induced platelet aggregation with an IC50 of 47 nM and haTRAP-induced platelet aggregation with an IC50 of 25 nM. Vorapaxar (SCH 530348) inhibits thrombininduced calcium transient in human coronary artery smooth muscle cells (HCASMC) with a Ki of 1.1 nM. It also inhibits thrombin-stimulated thymidine incorporation in HCASMC with a Ki of 13 nM.