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编 号：F350365
分子式：C24H21ClF4N8O2
分子量：564.92
分子式：C24H21ClF4N8O2
分子量：564.92
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CAS No: 405940-76-3
产品详情
生物活性：
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.
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 ID50 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 ID50 of 1.6 μmol/kg/h.
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 Ki of 0.16 nM.
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.
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 ID50 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 ID50 of 1.6 μmol/kg/h.
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 Ki of 0.16 nM.
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