BMS-986141 is a potent, selective antagonist of protease-activated receptor 4 (PAR4) with IC50 of 0.4 nM, Kd of 0.1 nM.
BMS-986141 potently inhibits platelet aggregation induced with a PAR4 agonist peptide (25 μM) with IC50 of 2.2 nM.
BMS-986141 shows no effect on platelet aggregation induced by a PAR1 antagonist peptide, adenosine diphosphate, collagen, or the thromboxane A2 receptor agonist U46619 up to 1 uM.
BMS-986141 (0.5 and 1 mg/kg) demonstrated excellent antithrombotic efficacy and minimal bleeding time prolongation in monkey models relative to the clinically important antiplatelet agent clopidogrel.
