货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V56712-1ml	10mM in DMSO	￥1100.00 V56712-1ml ￥1100.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V56712-1ml

10mM in DMSO

￥1100.00

货期：3-5天

产品描述：

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 [2] Target: AT1 receptor in 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

靶点：

Angiotensin Receptor

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。

参考文献：

1. Kajiya T, Ho C, Wang J, Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83. 2. Kusumoto K, Igata H, Ojima M, Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models. 3. Perry CM. Azilsartan medoxomil: a review of its use in hypertension. Clin Drug Investig. 2012 Sep 1;32(9):621-39. 4. Pierini D, Anderson KV. Azilsartan medoxomil/chlorthalidone: a new fixed-dose combination antihypertensive. Ann Pharmacother. 2013 May;47(5):694-703.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.648 ml	8.242 ml	16.485 ml
5 mM	0.33 ml	1.648 ml	3.297 ml
10 mM	0.165 ml	0.824 ml	1.648 ml
50 mM	0.033 ml	0.165 ml	0.33 ml

注意：

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参考文献

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Azilsartan kaMedoxoMil