BMS-986141

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BMS-986141

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1478711-48-6

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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。

生物活性

BMS-98614 is an orally active, selectivethrombinreceptorprotease-activated receptor-4 (PAR-4)antagonist with anIC₅₀value of 0.4 nM. BMS-98614 has excellent antithrombotic effect^[1]^[2].

IC₅₀& Target^[1]

PAR4

0.4 nM (IC₅₀)

体外研究
(In Vitro)

BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC₅₀value of 2.2 nM^[1].

体内研究
(In Vivo)

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

Clinical Trial

分子量

561.63

Formula

C₂₇H₂₃N₅O₅S₂

CAS 号

1478711-48-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.