Razaxaban,405940-76-3

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Razaxaban hydrochloride

CAS No. : 405940-76-3

MCE 国际站：Razaxaban hydrochloride

产品活性：Razaxaban hydrochloride (BMS 561389 hydrochloride) 是一种高效，选择性和口服活性的 factor Xa 抑制剂，K_i 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，K_i 为 540 nM。Razaxaban hydrochloride 具有很强的抗血栓形成活性。

研究领域：Metabolic Enzyme/Protease

作用靶点：Factor Xa  |  Thrombin

In Vitro: 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.

In Vivo: 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.

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