BMS-986141

Research use only, not for human use.

BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614 exhibits significant antithrombotic effects.

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.

BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC50 value of 2.2 nM.

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.

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GPCR/G Protein

PAR

Protease-activated Receptor

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1478711-48-6

561.63

C27H23N5O5S2

>98% (HPLC)

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O(CC=1N=C(SC1)C2=CC=C(C(N(C)C)=O)C=C2)C3=C4C(OC(=C4)C5=CN6C(=N5)SC(OC)=N6)=CC(OC)=C3

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(-20℃)

With Ice Pack

≥ 2 years