Razaxaban (Hydrochloride)
| 中文名称 | Razaxaban (Hydrochloride) |
|---|---|
| 中文同义词 | 化合物 T12694;化合物 RAZAXABAN HYDROCHLORIDE |
| 英文名称 | Razaxaban (Hydrochloride) |
| 英文同义词 | BMS 561389;Razaxaban (Hydrochloride);2-(3-amino-1,2-benzoxazol-5-yl)-N-[4-[2-[(dimethylamino)methyl]imidazol-1-yl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide:hydrochloride;DPC 906;DPC906;BMS 561389 hydrochloride;DPC 906 hydrochloride |
| CAS号 | 405940-76-3 |
| 分子式 | C24H21ClF4N8O2 |
| 分子量 | 564.9225528 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 405940-76-3.mol |
| 结构式 |  |
Razaxaban (Hydrochloride) 性质
Ki: 0.19 nM (Factor Xa); 540 nM (Thrombin)
Razaxaban (compound 11d) shows good Caco-2 permeability.
The anticoagulant activity of Razaxaban (compound 11d) is evaluated in the in vitro human plasma activated partial thromboplastin time (aPTT) and human prothrombin time (PT) assays. Razaxaban shows a doubling of aPTT and PT at 6.1 µM and 2.1 µM, respectively. The human and rabbit plasma protein binding are found to be 90.5% and 93.4%, respectively, using equilibrium dialysis. Razaxaban is found to have similar affinity in the rabbit factor Xa assay with a K
i
of 0.16 nM.
Razaxaban (Compound 11d; 0.21-9.4 mg/kg/hour; intravenous injection) inhibits thrombus formation in a dose-dependent manner with an ID 50 of 1.6 µmol/kg/h in the rabbit arterio-venous shunt thrombosis model.
| Animal Model: | Rabbit arterio-venous shunt thrombosis model |
| Dosage: | 0.21 mg/kg/hour, 0.7 mg/kg/hour, 2.1 mg/kg/hour, 9.4 mg/kg/hour |
| Administration: | Intravenous injection |
| Result: | Inhibited thrombus formation in a dose-dependent manner with an ID 50 of 1.6 µmol/kg/h. |