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抑制剂/激活剂

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凋亡与自噬

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Apixaban 阿哌沙班

Apixaban是一种高度选择性的，可逆的Factor Xa抑制剂，在人和兔子中Ki分别为0.08 nM和0.17 nM。

货号：
TK0564
规格：

1mg

5mg
价格：
￥0.00

产品参数

CAS No.	503612-47-3
生物活性	Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.
分子式	C25H25N5O4
分子量	459.5
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : 50 mg/mL (108.81 mM; Need ultrasonic)，H2O : < 0.1 mg/mL (insoluble)
体内研究	Apixaban (BMS-562247-01) shows the excellent pharmacokinetics with very low clearance (Cl: 0.02 L/kg/h), and low volume of distribution (Vdss: 0.2 L/kg) in the dogs. Besides, Apixaban also exhibits a moderate half-life (T1/2: 5.8 hours) and good oral bioavailability (F: 58%).In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produces dose-dependent antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM, respectively.Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo.In chimpanzee, Apixaban also shows small volume of distribution (Vdss: 0.17 L/kg), low systemic clearance (Cl: 0.018 L/kg/h), and good oral bioavailability (F: 59%).
体外研究	Apixaban (BMS-562247-01) prolongs the clotting times of normal human plasma with the concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays.
纯度及产品资料	98%

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