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5-R-Rivaroxaban
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。
5-R-Rivaroxaban图片
CAS NO:865479-71-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
5-R-Rivaroxaban 是一种 Rivaroxaban 的 R 型对映体。其中 Rivaroxaban 是选择性的Factor Xa(FXa) 抑制剂。

产品描述

5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor (IC50 0.7 nM; Ki 0.4 nM).

体外活性

Rivaroxaban competitively inhibits human FXa (Ki 0.4 nM) with >10 000-fold greater selectivity than for other serine proteases; it also inhibits prothrombinase activity (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa more potently in human and rabbit plasma (IC50 21 nM) than rat plasma (IC50 290 nM). It demonstrates anticoagulant effects in human plasma, doubling prothrombin time (PT) and activates partial thromboplastin time at 0.23 and 0.69 μM, respectively [2].

体内活性

Rivaroxaban, administered by i.v. bolus before thrombus induction, reduces thrombus formation (ED50 0.1 mg/kg), inhibits FXa, and prolongs PT dose-dependently. PT and FXa are affected slightly at the ED50 (1.8-fold increase and 32% inhibition, respectively). At 0.3 mg/kg (dose leading to almost complete inhibition of thrombus formation), Rivaroxaban moderately prolongs PT (3.2±0.5-fold) and inhibits FXa activity (65±3%) [2].

Cas No.

865479-71-6

分子式

C19H18ClN3O5S

分子量

435.88

储存和溶解度

DMSO:33.33 mg/mL (76.47 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years