生物活性 | |||
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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]. |
实验方案 | |||
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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 |
参考文献 |
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