BMS-98614 是一种口服活性的、选择性的凝血酶受体蛋白酶激活受体-4 (PAR-4) (Protease-activated Receptor-4 (PAR-4)) 拮抗剂，其IC50值为 0.4 nM。BMS-98614 具有优异的抗血栓功效。

BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC 50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect [1] [2].

BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC 50 value of 2.2 nM [1].

BMS-986141 (compound 49) shows a slight but significant prolongation of KBT (kidney bleeding time) and demonstrates excellent anti-thrombotic efficacy at 0.5 mg/kg in cynomolgus monkey [1] [2]. Animal Model: Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models [2] Dosage: 0.05, 0.1, 0.5 mg/kg Administration: p.o., 2 hours Result: Inhibited PAR4-AP-induced platelet aggregation in human and monkey blood with IC50 of 1.8 and 1.3 nM, respectively. Reduced the thrombus weight by 36%, 63% and 88% at concentrations of 0.05, 0.1 and 0.5 mg/kg, respectively in AT model. Increased MBT by 1.2 times. Animal Model: Rat, dog and monkey [1] Dosage: 0.5, 1, 2 mpk Administration: i.v., 0.5 mpk, 10 min or p.o., 2 mpk for rat, 1 mpk for dog and monkey Result: The pharmacokinetic parameters of BMS-986141 (compound 49) Parameters rat dog monkey t 1/2 (h) 3.7 ± 0.4 13 75 ± 12 CL (mL/min/kg) 14.3 ± 0.4 8.5 12 ± 2 Vss(L/kg) 2.7 ± 0.3 2.7 14 ± 5 F (%) 31 25 36

1478711-48-6

C27H23N5O5S2

561.63

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years