BMS 986120

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). 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.Formal Name: 2-methoxy-6-[6-methoxy-4-[[5-methyl-2-(4-morpholinyl)-4-thiazolyl]methoxy]-2-benzofuranyl]-imidazo[2,1-b]-1,3,4-thiadiazole. CAS Number: 1478712-37-6. Molecular Formula: C23H23N5O5S2. Formula Weight: 513.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. lambdamax: 305 nm. SMILES: COC1=CC2=C(C=C(C3=CN4C(SC(OC)=N4)=N3)O2)C(OCC5=C(C)SC(N6CCOCC6)=N5)=C1. InChi Code: InChI=1S/C23H23N5O5S2/c1-13-17(25-21(34-13)27-4-6-31-7-5-27)12-32-18-8-14(29-2)9-19-15(18)10-20(33-19)16-11-28-22(24-16)35-23(26-28)30-3/h8-11H,4-7,12H2,1-3H3. InChi Key: MINMDCMSHDBHKG-UHFFFAOYSA-N.