Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Azilsartan Medoxomil Potassium (TAK-491 Potassium) 是一种具有口服活性的1型血管紧张素 II 受体拮抗剂(IC50: 0.62 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 917 | 现货 | ||
5 mg | ¥ 1,960 | 现货 | ||
10 mg | ¥ 3,250 | 现货 | ||
25 mg | ¥ 5,980 | 现货 | ||
50 mg | ¥ 8,780 | 现货 | ||
100 mg | ¥ 11,800 | 现货 |
产品描述 | Azilsartan Medoxomil Potassium (TAK-491 Potassium) 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. |
体外活性 | Azilsartan Medoxomil Potassium is a prodrug, which is rapidly converted to the active moiety, azilsartan (TAK-536), by ester hydrolysis in the gut and plasma during absorption after oral administration. Azilsartan selectively blocks the binding of angiotensin II to the AT1 (angiotensin II type 1) receptors found in the vascular smooth muscle and the adrenal gland, thereby promoting vasodilation and a decrease in the effects of aldosterone. Azilsartan is a highly selective antagonist to the AT1 receptor, with an IC50 of 2.6 nM, exhibiting a >10,000-fold affinity for the AT1 receptor compared with the AT2 receptor, and has not shown affinity for other cardiac receptors or ion channels[1]. The inhibitory effect of Azilsartan persists after washout of the free compound (IC50 value of 7.4 nM). Azilsartan also inhibits the accumulation of angiotensin II -induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM, and this effect is resistant to washout (IC50 value of 81.3 nM)[1]. |
别名 | TAK-491 Potassium |
分子量 | 606.62 |
分子式 | C30H23N4O8·K |
CAS No. | 863031-24-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Soluble
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Azilsartan Medoxomil Potassium 863031-24-7 TAK-491 Potassium Azilsartan kaMedoxoMil Inhibitor inhibitor inhibit