CAS:330942-05-7Betrixaban

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Synonyms: PRT-054021

Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM (inhibition of Factor 10a).

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18817579266

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实验数据

技术信息

CAS号

330942-05-7

储存条件

分子式

C23H22ClN5O3

运输

蓝冰

分子量

451.91

别名

PRT-054021

溶解度

DMSO	59.0 mg/mL (130.6 mM) warming
Water	insoluble

动物实验配方

生物活性

描述Serine protease factor Xa (fXa), positioned at the juncture of the intrinsic and the extrinsic pathways, play a pivotal role in the blood coagulation cascade. Betrixaban is a highly potent, selective, and orally efficacious fXa inhibitor with IC50of 1.5 nM. In patch clamp hERG (human ether-a-go-go related gene) assays, Betrixaban has IC50 value of 8.9 μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki⩽0.5 μM). Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey. After i.v. infusion for 30 min, the total plasma concentration of Betrixaban is 0.2±0.01 μM, and the percentage of unbound inhibitor is 40%±7.2%.
作用机制The chloropyridine A ring extents into the fXa S1 site with the chloro atom positioned above the phenyl ring of Tyr228 and occupies a hydrophobic pocket formed by Ala190, Val213 and Tyr228.