405940-76-3
405940-76-3 結(jié)構(gòu)式
基本信息
化合物 RAZAXABAN HYDROCHLORIDE
DPC 906
BMS 561389
DPC 906 hydrochloride
BMS 561389 hydrochloride
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
常見問題列表
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. |