• Catalog Number:

  E1KS3002

• Amount:

  5mg1​ PHYSICAL AND CHEMICAL PROPERTIES

HYPERLINK "http://www.selleckchem.com/../pic/digi/S3002.gif" \t "_blank" 2​ Biological Activity A novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders. Rivaroxaban inhibits clot-associated,free FXa activity,and prothrombinase activity, in addition, it reduces thrombin generation. The activated serine protease Factor Xa (FXa) plays a central role in the blood coagulation cascade. FXa catalyzes the conversion of prothrombin to thrombin through the prothrombinase complex, which consists of FXa, FVa, prothrombin, and Ca2+ on a phospholipid surface. Thrombin has several thrombotic functions, including the conversion of fibrinogen to fibrin, the activation of platelets, and the feedback activation of other coagulation factors, resulting in the amplification of its own formation. [1] At concentrations up to 20μM, Rivaroxaban(Xarelto) did not affect related serine proteases; selectivity was more than 10000-fold greater for FXa. BAY 59-7939 showed a similar affinity to purified human and rabbit FXa (IC50=0.7 ± 0.01 and 0.8 ± 0.01 ηM, respectively),but was less potent against purified rat FXa (IC50 3.4 ηM). In plasma, endogenous human and rabbit FXa, generated by RVV, was inhibited to a similar extent by BAY 59-7939 (IC50=21 ± 0.001 and 21 ± 0.002 ηM, respectively), whereas 14-fold higher concentrations were required in rat plasma (IC50=290 ± 0.02 ηM). [2] 3​ References: [1] Roehrig S et al. J Med Chem. 2005 Sep 22;48(19):5900-8 [2] Perzborn Eet al. J Thromb Haemost. 2005 Mar; 3(3):514-21 The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.