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编 号：F485523
分子式：C30H23KN4O8
分子量：606.62
分子式：C30H23KN4O8
分子量：606.62
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CAS No: 863031-24-7
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生物活性：
Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. IC50 Value: 0.62 nM Target: AT1 receptorin vitro: In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors.in vivo: Oral administration of 0.1-3 mg/kg olmesartan medoxomil reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively . Over a longer treatment period of 24 weeks, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP at week 24 significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan 320 mg once daily. Mean reductions from baseline in mean clinic SBP and DBP as well as DBP by ABPM were also significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan. In 4 randomized controlled trials (3 published to date), azilsartan medoxomil/chlorthalidone 40 mg/12.5 mg and 40 mg/25 mg reduced blood pressure (BP) significantly more than comparators did, including an approximately 5-mm Hg greater BP reduction than olmesartan medoxomil/hydrochlorothiazide 40 mg/25 mg and azilsartan medoxomil/hydrochlorothiazide .
体内研究：
Azilsartan medoxomil (0.03-1 mg/kg，口服) monopotassium 抑制正常血压大鼠中血管紧张素 II 诱导的升压反应。Azilsartan medoxomil (花生酱中 0.1-10 mg/kg，每日一次) monopotassium 抑制 I 型纤溶酶原激活剂抑制剂 (PAI-1) 蛋白的血管壁表达，并可能促进 ApoE 敲除小鼠 (高脂饮食) (VSMC 中 PAI-1 过度表达) 动脉粥样硬化斑块的稳定 。Azilsartan medoxomil (0.03-10 mg/kg，口服灌胃，每天一次) monopotassium 可减少大鼠心肌梗死面积。
Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. IC50 Value: 0.62 nM Target: AT1 receptorin vitro: In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors.in vivo: Oral administration of 0.1-3 mg/kg olmesartan medoxomil reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively . Over a longer treatment period of 24 weeks, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP at week 24 significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan 320 mg once daily. Mean reductions from baseline in mean clinic SBP and DBP as well as DBP by ABPM were also significantly greater with azilsartan medoxomil 40 or 80 mg once daily than with valsartan. In 4 randomized controlled trials (3 published to date), azilsartan medoxomil/chlorthalidone 40 mg/12.5 mg and 40 mg/25 mg reduced blood pressure (BP) significantly more than comparators did, including an approximately 5-mm Hg greater BP reduction than olmesartan medoxomil/hydrochlorothiazide 40 mg/25 mg and azilsartan medoxomil/hydrochlorothiazide .
体内研究：
Azilsartan medoxomil (0.03-1 mg/kg，口服) monopotassium 抑制正常血压大鼠中血管紧张素 II 诱导的升压反应。Azilsartan medoxomil (花生酱中 0.1-10 mg/kg，每日一次) monopotassium 抑制 I 型纤溶酶原激活剂抑制剂 (PAI-1) 蛋白的血管壁表达，并可能促进 ApoE 敲除小鼠 (高脂饮食) (VSMC 中 PAI-1 过度表达) 动脉粥样硬化斑块的稳定 。Azilsartan medoxomil (0.03-10 mg/kg，口服灌胃，每天一次) monopotassium 可减少大鼠心肌梗死面积。
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