CAS NO: | 366789-02-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Rivaroxaban (BAY 59-7939) is a highly potent, selective and directFactor Xa(FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC500.7 nM;Ki0.4 nM)[1][2]. | ||||||||||||||||
IC50& Target | IC50: 0.7 nM (FXa)[1] | ||||||||||||||||
体外研究 (In Vitro) | Rivaroxaban (BAY 59-7939) is an oral, direct Factor Xa (FXa) inhibitor in development for the prevention and treatment of arterial and venous thrombosis. Rivaroxaban competitively inhibits human FXa (Ki0.4 nM) with >10 000-fold greater selectivity than for other serine proteases; it also inhibits prothrombinase activity (IC502.1 nM). Rivaroxaban inhibits endogenous FXa more potently in human and rabbit plasma (IC5021 nM) than rat plasma (IC50290 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]. | ||||||||||||||||
体内研究 (In Vivo) | Rivaroxaban (BAY 59-7939) is a potent and selective, direct FXa inhibitor with excellent in vivo activity and good oral bioavailability[1]. Rivaroxaban (BAY 59-7939), administered by i.v. bolus before thrombus induction, reduces thrombus formation (ED500.1 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 435.88 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H18ClN3O5S | ||||||||||||||||
CAS 号 | 366789-02-8 | ||||||||||||||||
中文名称 | 利伐沙班;立伐沙班 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(114.71 mM;Need ultrasonic) 配制储备液
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