阿齐沙坦酯 T6219
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
1 mg | 863031-21-4 | ¥279.00 | 询底价 |
5 mg | 863031-21-4 | ¥828.00 | 询底价 |
1 mL | 863031-21-4 | ¥987.00 | 询底价 |
2 mg | 863031-21-4 | ¥397.00 | 询底价 |
100 mg | 863031-21-4 | ¥5,330.00 | 询底价 |
10 mg | 863031-21-4 | ¥1,230.00 | 询底价 |
25 mg | 863031-21-4 | ¥2,260.00 | 询底价 |
50 mg | 863031-21-4 | ¥3,730.00 | 询底价 |
500 mg | 863031-21-4 | ¥10,800.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Azilsartan Medoxomil
描述: 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)。
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)
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.
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]
存储条件: 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)
关键字: TAK 491 | TAK491 | Inhibitor | inhibit | Angiotensin Receptor | Azilsartan Medoxomil
相关产品: Angiotensin II human acetate | BIBS 39 | Perindoprilat | Ceronapril | Lisinopril | Eprosartan | Methyl candesartan | Valsartan Methyl Ester | Saralasin acetate(34273-10-4 free base) | Buloxibutid
相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Anti-Hypertension Compound Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Highly Selective Inhibitor Library | EMA Approved Drug Library | Endocrinology-Hormone Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途