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编 号：F745487
分子式：C27H23N5O5S2
分子量：561.63
分子式：C27H23N5O5S2
分子量：561.63
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CAS No: 1478711-48-6
产品详情
生物活性：
BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect.
体内研究：
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.Animal Model:Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models
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
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) Parametersratdog monkey
t1/2(h)3.7 ± 0.41375 ± 12
CL (mL/min/kg)14.3 ± 0.48.512 ± 2
Vss(L/kg)2.7 ± 0.32.714 ± 5
F (%)312536
体外研究：
BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC50 value of 2.2 nM.
BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect.
体内研究：
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.Animal Model:Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models
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
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) Parametersratdog monkey
t1/2(h)3.7 ± 0.41375 ± 12
CL (mL/min/kg)14.3 ± 0.48.512 ± 2
Vss(L/kg)2.7 ± 0.32.714 ± 5
F (%)312536
体外研究：
BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC50 value of 2.2 nM.
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