405940-76-3

中文名称 Razaxaban (Hydrochloride)

英文名称 Razaxaban (Hydrochloride)

CAS 405940-76-3

分子式 C24H21ClF4N8O2

分子量 564.923

MOL 文件 405940-76-3.mol

405940-76-3 结构式

基本信息常见问题列表

基本信息

中文别名

化合物 T12694
化合物 RAZAXABAN HYDROCHLORIDE

英文别名

DPC906
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

常见问题列表

生物活性

Razaxaban hydrochloride (BMS 561389 hydrochloride) 是一种高效，选择性和口服活性的 factor Xa 抑制剂，Ki 为 0.19 nM。Razaxaban hydrochloride 对 factor Xa 的选择性优于其他相关丝氨酸蛋白酶 (> 5000 倍)。Razaxaban hydrochloride 也是一种有效的凝血酶抑制剂，Ki 为 540 nM。Razaxaban hydrochloride 具有很强的抗血栓形成活性。

靶点

Ki: 0.19 nM (Factor Xa); 540 nM (Thrombin)

体外研究

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.

体内研究

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.