Rivaroxaban

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 ´µM, 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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