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Azilsartan Medoxomil

Azilsartan Medoxomil

产品编号 T6219   CAS 863031-21-4
别名: TAK-491, 阿齐沙坦酯

Azilsartan Medoxomil (TAK-491) 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)。

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Azilsartan Medoxomil Chemical Structure
Azilsartan Medoxomil, CAS 863031-21-4
规格 价格/CNY 货期 数量
1 mg ¥ 279 现货
2 mg ¥ 397 现货
5 mg ¥ 828 现货
10 mg ¥ 1,230 现货
25 mg ¥ 2,260 现货
50 mg ¥ 3,730 现货
100 mg ¥ 5,330 现货
500 mg ¥ 10,800 现货
1 mL * 10 mM (in DMSO) ¥ 987 现货
产品目录号及名称: Azilsartan Medoxomil (T6219)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Azilsartan Medoxomil (TAK-491) 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.
靶点活性 angiotensin II receptor type 1:0.62 nM
体外活性 Azilsartan medoxomil 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. [2] 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. 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]
激酶实验 Radioligand Binding: A radioligand binding assay is performed by using human AT1 receptor-coated microplates containing 4.4 to 6.2 fmol of receptors/well (10 μg of membrane protein/well). Membrane-coated wells are incubated with 45 μl of assay buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, and 0.005% CHAPS, pH 7.4) containing various concentrations of test compounds at room temperature. After 90 min, 5 μl of 125I-Sar1-Ile8-AII (final concentration 0.6 nM) dissolved in assay buffer is added to the wells, and the plate is incubated for 5 h. In each step, the plate is briefly and gently shaken on a plate shaker.
细胞实验 Measurement of Inositol 1-Phosphate Accumulation. Twentyfour hours after transfections with human AT1-expressing plasmids, the cells are starved by changing the culture medium to starvation buffer (1 mM CaCl2, 0.5 mM MgCl2, 4.2 mM KCl, 146 mM NaCl, 5.5 mM glucose, and 10 mM HEPES, pH 7.3). Then, 5 μl/well of the test compounds dissolved in starvation buffer is added to the cells at the indicated concentrations, and they are pretreated for the indicated times. Two hours after starvation, LiCl is added to a final concentration of 50 mM with or without angiotensin II 10 nM, and the cells are further incubated for the indicated times at 37°C. In washout experiments, the cells are washed once with 100 μl/well of starvation buffer to remove unbound compounds before stimulation with angiotensin II. The accumulation of inositol 1-phosphate (IP1) is measured by using a IP-One Tb kit. The fluorescence resonance energy transfer signal is measured on a plate reader.(Only for Reference)
别名 TAK-491, 阿齐沙坦酯
分子量 568.53
分子式 C30H24N4O8
CAS No. 863031-21-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 105 mg/mL (184.7 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7589 mL 8.7946 mL 17.5892 mL 43.9731 mL
5 mM 0.3518 mL 1.7589 mL 3.5178 mL 8.7946 mL
10 mM 0.1759 mL 0.8795 mL 1.7589 mL 4.3973 mL
20 mM 0.0879 mL 0.4397 mL 0.8795 mL 2.1987 mL
50 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
100 mM 0.0176 mL 0.0879 mL 0.1759 mL 0.4397 mL

计算器

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参考文献

1. Ojima M, et al. J Pharmacol Exp Ther, 2011, 336(3), 801-808. 2. Zaiken K, et al. Clin Ther, 2011, 33(11), 1577-1589.

文献引用

1. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866.
Delapril hydrochloride Sinapinic Acid Angiotensin II human H-Val-Pro-Pro-OH Fimasartan Zofenopril calcium Resorcinolnaphthalein Enalapril Maleate

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 儿童药物库 抑制剂库 临床期小分子药物库 上市药物库 抗心血管疾病化合物库 FDA 上市药物库 抗COVID-19化合物库 经典已知活性库 ReFRAME 相关化合物库

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体内实验配液计算器

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。

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技术支持

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。

Keywords

Azilsartan Medoxomil 863031-21-4 Endocrinology/Hormones RAAS TAK-491 TAK 491 TAK491 阿齐沙坦酯 Inhibitor inhibit Angiotensin Receptor inhibitor

 

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