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Rivaroxaban

CAS No. : 366789-02-8

MCE 國際站：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，K_i 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 (K_i 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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