CAS:366789-02-8Rivaroxaban

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Synonyms: BAY 59-7939

Rivaroxaban is an inhibitor of factor Xa (FXa) with IC50 of 0.7 nM and Ki of 0.4 nM which developed for the treatment of thrombotic disease.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

366789-02-8

储存条件

分子式

C19H18ClN3O5S

运输

蓝冰

分子量

435.88

别名

BAY 59-7939

溶解度

动物实验配方

0.5% methylcellulose+0.2% Tween 80+water

5 mg/mL

suspension

生物活性

描述The activated serine protease Factor Xa (FXa), activated by both the intrinsic and the extrinsic pathways, plays a central role in the blood coagulation cascade. FXa catalyzes the conversion of prothrombin tothrombin through the prothrombinase complex. Rivaroxaban, also called BAY 59-7939, is an inhibitor of FXa with IC₅₀ of 0.7 nM and Ki of 0.4 nM which is under clinical development for the treatment of thrombotic disease. Rivaroxaban (15, 30, or 60 ng/mL) inhibited thrombin generation in a concentration-dependent manner and the effect was enhanced with ticagrelor (1.0 µg/mL) and ticagrelor plus acetylsalicylic acid (100 µg/mL). Rivaroxaban (0.01, 0.03, or 0.1 mg/kg) also dose-dependently reduced thrombus formation in arteriovenous shunt model in rats. Oral rivaroxaban (2.5 mg twice-daily [bid] and 5 mg bid) reduced mortality and morbidity in patients with acute coronary syndrome, when combined with antiplatelets.
作用机制Rivaroxaban forms two hydrogen bonds to Gly219 of Factor Xa.