产品描述:
BMS 986120 is an orally bioavailable, selective, and reversible antagonist of proteinase-activated receptor 4 (PAR4; IC50 = 0.56 nM to inhibit calcium mobilization induced by PAR4 agonist peptide (PAR4-AP) in HEK293 cells).{36234} It is selective for PAR4 over PAR1, PAR2, and a panel of purified proteases, including thrombin. It inhibits platelet aggregation in vitro in human platelet-rich plasma (IC50 = 7.3 nM). BMS 986120 (0.2-1 mg/kg) decreases platelet aggregation induced by PAR4-AP ex vivo in a dose-dependent manner, but does not increase clotting times. In vivo, BMS 986120 (1 mg/kg) prevents vascular occlusion and reduces thrombus formation by 82% in cynomolgus monkeys.