Rivaroxaban

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M.Wt: 435.88 Formula: C19H18ClN3O5S Solubility: Soluble in DMSO, acetone, polyethylene glycol Purity: 99% Storage: -20C 2 years CAS No.: 366789-02-8

Biological Activity: It is the first available orally active direct inhibitor of coagulation Factor Xa. BAY 59-7939 competitively inhibits human FXa ( Ki 0.4 nM) with > 10 000-fold greater selectivity than for other serine proteases. it also inhibited prothrombinase activity ( IC50 2.1 nM) . BAY 59-7939 inhibited endogenous FXa more potently in human and rabbit plasma ( IC50 21 nM) than rat plasma ( IC50 290 nM) . It demonstrated anticoagulant effects in human plasma, doubling prothrombin time ( PT) and activated partial thromboplastin time at 0.23 and 0.69 µ M, respectively. In vivo, BAY 59-7939 reduced venous thrombosis ( fibrin-rich, platelet-poor thrombi) dose dependently ( ED50 0.1 mg/ kg i.v.) in a rat venous stasis model. BAY 59-7939 reduced arterial ( fibrinand platelet-rich) thrombus formation in an arteriovenous ( AV) shunt in rats ( ED50 5.0 mg / kg p.o.) and rabbits ( ED50 0.6 mg/ kg p.o.) . Slight inhibition of FXa ( 32% at ED50) reduced thrombus formation in the venous model; to affect arterial thrombosis in the rat and rabbit, stronger inhibition of FXa ( 74% , 92% at ED50) was required. Rivaroxaban is well absorbed from the gut and maximum inhibition of factor Xa occurs three hours after a dose. The effects lasts 8-12 hours, but factor Xa activity does not return to normal within 24 hours so once-daily dosing is possible.

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