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5-R-利伐沙班 /5-R-Rivaroxaban {[allProObj[0].p_purity_real_show]}

货号:A785317 Ambeed 开学季,买赠积分,赢豪礼

5-R-Rivaroxaban is an (R) enantiomer of rivaroxaban, an oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders.

5-R-Rivaroxaban 化学结构 CAS号:865479-71-6
5-R-Rivaroxaban 化学结构
CAS号:865479-71-6
5-R-Rivaroxaban 3D分子结构
CAS号:865479-71-6
5-R-Rivaroxaban 化学结构 CAS号:865479-71-6
5-R-Rivaroxaban 3D分子结构 CAS号:865479-71-6
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5-R-Rivaroxaban 纯度/质量文件 产品仅供科研

货号:A785317 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Factor Xa 其他靶点 纯度
Rivaroxaban ++

Factor Xa, IC50: 0.7 nM

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Apixaban ++++

Factor Xa (human), Ki: 0.08 nM

Factor Xa (rabbit), Ki: 0.17 nM

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Edoxaban tosylate monohydrate +++

Factor Xa, Ki: 0.561 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

5-R-Rivaroxaban 生物活性

描述 Rivaroxaban (BAY 59-7939) is being developed as an oral, direct inhibitor of Factor Xa (FXa) for the prevention and treatment of both arterial and venous thrombosis. It competitively inhibits human FXa with a Ki of 0.4 nM, demonstrating over 10,000 times greater selectivity over other serine proteases and inhibits prothrombinase activity with an IC50 of 2.1 nM. In human and rabbit plasma, Rivaroxaban more potently inhibits endogenous FXa (IC50 21 nM) compared to rat plasma (IC50 290 nM). It effectively doubles prothrombin time and activates partial thromboplastin time at concentrations of 0.23 μM and 0.69 μM, respectively, indicating its anticoagulant effects[2].
体内研究

Rivaroxaban (BAY 59-7939) is a highly potent and selective FXa inhibitor that exhibits excellent in vivo activity and favorable oral bioavailability[1].

Administered intravenously before thrombus induction, Rivaroxaban significantly reduces thrombus formation with an ED50 of 0.1 mg/kg, dose-dependently inhibits FXa, and prolongs prothrombin time. At the ED50, PT is modestly increased (1.8-fold) and FXa activity is inhibited by 32%. At a dose of 0.3 mg/kg, which nearly completely prevents thrombus formation, Rivaroxaban prolongs PT by 3.2±0.5-fold and inhibits 65±3% of FXa activity[2].

体外研究

Rivaroxaban (BAY 59-7939) is being developed as an oral, direct inhibitor of Factor Xa (FXa) for the prevention and treatment of both arterial and venous thrombosis. It competitively inhibits human FXa with a Ki of 0.4 nM, demonstrating over 10,000 times greater selectivity over other serine proteases and inhibits prothrombinase activity with an IC50 of 2.1 nM. In human and rabbit plasma, Rivaroxaban more potently inhibits endogenous FXa (IC50 21 nM) compared to rat plasma (IC50 290 nM). It effectively doubles prothrombin time and activates partial thromboplastin time at concentrations of 0.23 μM and 0.69 μM, respectively, indicating its anticoagulant effects[2].

5-R-Rivaroxaban 参考文献

[1]Roehrig S, et al. Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor. J Med Chem. 2005 Sep 22;48(19)

[2]Perzborn E, et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor. J Thromb Haemost. 2005 Mar;3(3):514-21.

5-R-Rivaroxaban 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.47mL

2.29mL

1.15mL

22.94mL

4.59mL

2.29mL

5-R-Rivaroxaban 技术信息

CAS号865479-71-6
分子式C19H18ClN3O5S
分子量 435.881
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(80.3 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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