目錄:MedChemExpress LLC>>信號(hào)通路>> Rivaroxaban | MedChemExpress
參考價(jià) | ¥ 715 |
參考價(jià) | ¥ 715 |
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CAS | 366789-02-8 | 純度 | 99.84% |
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分子量 | 435.88 | 分子式 | C??H??ClN?O?S |
供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
貨號(hào) | HY-50903 | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥 |
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CAS No. : 366789-02-8
MCE 國(guó)際站:Rivaroxaban
產(chǎn)品活性:Rivaroxaban 是一種高效,選擇性直接的凝血因子 Xa (FXa) 抑制劑,IC50 為 0.7 nM,Ki 為 0.4 nM。
研究領(lǐng)域:Metabolic Enzyme/Protease
作用靶點(diǎn):Factor Xa
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 (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.
In Vivo: Rivaroxaban (BAY 59-7939) is a potent and selective, direct FXa inhibitor with excellent in vivo activity and good oral bioavailability. Rivaroxaban (BAY 59-7939), 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%).
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