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 drμg transport up to concentrations of 100 μM in vitro. 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.
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Rivaroxaban
Dangerous GoodsCAS number：366789-02-8 molecular formula：C19H18ClN3O5S
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Specs
| Chinese alias | 利伐沙班 | ||
| English alias | B01AF01 | 1429742-50-6 | 2-Thiophenecarboxamide, 5-chloro-N-(((5S)-2-oxo-3-(4-(3-oxo-4-morpholinyl)phenyl)-5-oxazolidinyl)methyl)- | 2w26 | 9NDF7JZ4M3 | Q420262 | Xarelto | MFCD11974010 | N-Smc-carboxylate | L-Glutatione | RIVAROXABAN [ORANGE BOOK] | MLS0 | ||
| CAS number | 366789-02-8 | molecular formula | C19H18ClN3O5S |
| molecular weight | 435.88 g/mol | Exact mass | - |
| PSA | 116.000 Ų | logp | 2.5 |
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Safety information
pictogram：
GHS09
Hazard Statement：
H411: 对水生生物有毒并具有长期持续影响
Statement of Preventive Measures：
P273: 避免释放到环境中。 P501: 将内容物/容器处理到。。。 P391: 收集溢出物
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MSDS
Found 1 shareMSDS
366789-02-8 | Rivaroxaban CRS.pdf
