Product Overview
5-R-Rivaroxaban is a selective inhibitor of human Factor Xa with IC50 value of 0.7 nmol/L. Factor Xa is a serine endopeptidase enzyme and plays an important role in the convergence point of the intrinsic and extrinsic pathways in blood coagulation system. 5-R-Rivaroxaban is an oral, direct factor Xa inhibitor and the inhibition is species-dependent. When tested with purified factoe Xa from human or rabbit, 5-R-Rivaroxaban showed similar affinity with IC50 value of 0.7 nmol/L and 0.8 nmol/L, respectively, while had a IC50 value as low as 3.4 nmol/L when tested with rat factor Xa. Pre-treated anaesthetised rat model with intravenous 5-R-Rivaroxaban at a dose of 2 mg/kg, and after bleeding initiated intravenous treated with rFVIIa (100/400 μg/kg), PCC (25/50 U/kg) or aPCC (50/100 U/kg), the result showed that 5-R-Rivaroxaban pre-treatment significantly shorten bleeding time and clotting time compared with 5-R-Rivaroxaban alone treated group. Similar results were obtained when tested with rabbit model. It has been reported that 5-R-Rivaroxaban is a promising drug for atrial fibrillation, venous thromboembolism or thromboembolic disorders in clinic.