Razaxaban (Hydrochloride)
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- CAS号:
- 405940-76-3
- 英文名:
- 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
- 中文名:
- Razaxaban (Hydrochloride)
- 中文别名:
- 化合物 T12694
- CBNumber:
- CB62627607
- 分子式:
- C24H21ClF4N8O2
- 分子量:
- 564.9225528
- MOL File:
- 405940-76-3.mol
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Razaxaban (Hydrochloride)化学性质
Razaxaban (Hydrochloride)性质、用途与生产工艺
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。
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.
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Animal Model:
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Rabbit arterio-venous shunt thrombosis model
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Dosage:
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0.21 mg/kg/hour, 0.7 mg/kg/hour, 2.1 mg/kg/hour, 9.4 mg/kg/hour
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Administration:
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Intravenous injection
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Result:
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Inhibited thrombus formation in a dose-dependent manner with an ID
50
of 1.6 µmol/kg/h.
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Razaxaban (Hydrochloride)
上下游产品信息
上游原料
下游产品
Razaxaban (Hydrochloride)
生产厂家
405940-76-3, Razaxaban (Hydrochloride) 相关搜索:
- 化合物 T12694
- 405940-76-3
- 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
- Razaxaban (Hydrochloride)
- BMS 561389