Rivaroxaban

A highly potent and selective, direct FXa inhibitor with IC50 of 0.7 nM; displays >10,000-fold greater selectivity than for other serine proteases, also inhibits prothrombinase activity (IC50=2.1 nM) ; inhibits endogenous FXa more potently in human than rat plasma (IC50 21 nM vs 290 nM) ; reduces venous thrombosis dose dependently (ED50=0.1 mg/kg i.v.) in a rat venous stasis model; orally active.Thrombosis Approved (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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BAY 59-7939

Pharmacology & Drug Discovery

>98% (HPLC)

10 mM in DMSO

O=C (C1=CC=C (Cl) S1) NC[C@H]2CN (C3=CC=C (N4C (COCC4) =O) C=C3) C (O2) =O

C19H18ClN3O5S

435.8813

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.