产品描述
| 溶解性 |
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| 存贮条件 | 储存温度-20°C |
| 产品介绍 | Rivaroxaban is an oral, direct inhibitor of Factor X, being developed for the prevention and treatment of arterial and venous thrombosis with a Ki of 0.4 nM. Rivaroxaban also inhibits prothrombinase activity (IC50 = 2.1 nM). Rivaroxaban also shows a similar affinity to purified human (IC50 = 0.7 nM) and rabbit Factor X (IC50 = 0.8 nM), but a lesser potency against purified rat Factor X (IC50 = 3.4 nM). Endogenous human and rabbit Factor X in plasma is inhibited to a similar extent by Rivaroxaban (IC50 = 21 nM and 21 nM, respectively), while 14-fold higher concentrations are required in rat plasma (IC50 = 290 nM). Rivaroxaban exhibits high permeability and polarized transport across Caco-2 cells as a substrate of the P-gp, but exhibits no inhibitory effect on P-gp-mediated drug transport up to concentrations of 100 μM in vitro. |
| 备注 | Rivaroxaban is a direct inhibitor of Factor Xa with Ki and IC50 of 0.4 nM and 0.7 nM, respectively. |
| 生化机理 |
Rivaroxaban (Xarelto; BAY 59-7939) is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders. Rivaroxaban (Xarelto; BAY 59-7939) inhibits clot-associated,free FXa activity,and prothrombinase activity, in addition, it reduces thrombin generation. Rivaroxaban (Xarelto; BAY 59-7939) is useful for antithrombotic agent |
| 别名 | 利伐沙班;(S)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide |
