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Azilsartan medoxomil/阿齐沙坦酯 {[allProObj[0].p_purity_real_show]}

货号:A325842 同义名: TAK-491

Azilsartan Medoxomil is an orally available angiotensin II type 1 (AT1) receptor antagonist with IC50 value of 2.6 nM.

Azilsartan medoxomil/阿齐沙坦酯 化学结构 CAS号:863031-21-4
Azilsartan medoxomil/阿齐沙坦酯 化学结构
CAS号:863031-21-4
Azilsartan medoxomil/阿齐沙坦酯 3D分子结构
CAS号:863031-21-4
Azilsartan medoxomil/阿齐沙坦酯 化学结构 CAS号:863031-21-4
Azilsartan medoxomil/阿齐沙坦酯 3D分子结构 CAS号:863031-21-4
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Azilsartan medoxomil/阿齐沙坦酯 纯度/质量文件 产品仅供科研

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Azilsartan medoxomil/阿齐沙坦酯 生物活性

靶点
  • AT1 receptor

    AT1 receptor, IC50:2.6 nM

描述 Azilsartan Medoxomil, a new angiotensin II Type 1 receptor blockers with IC50 of 0.62 nM. In conscious spontaneously hypertensive rats (SHRs), oral administration of 0.1-1mg/kg azilsartan medoxomil significantly reduced blood pressure at all doses even 24h after dosing[3]. Azilsartan medoxomil, in 40 and 80 mg doses, combined with 5 mg of the calcium channel blocker amlodipine was well tolerated and led to meaningful additional BP(blood pressure) reductions compared with placebo plus amlodipine[4]. Further, in aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l. Antiproliferative effects of azilsartan were also observed in cells lacking AT1(angiotensin II type 1) receptors[5].

Azilsartan medoxomil/阿齐沙坦酯 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01715584 Hypertension Phase 4 Recruiting December 31, 2019 Canada, Ontario ... 展开 >> London Health Sciences Centre - Victoria Campus Recruiting London, Ontario, Canada, N6A 5W9 Contact: Craig J Railton, MD, PhD    519 685 8500 ext 58525    Craig.Railton@lhsc.on.ca    Principal Investigator: Craig J Railton, MD, PhD          Sub-Investigator: Jonathan Fairbairn, BSc          Sub-Investigator: George Nicoloau, MD          Sub-Investigator: Robert Gros, PhD          Sub-Investigator: Jason Franklin, MD          Sub-Investigator: John Yoo, MD          Sub-Investigator: Kevin Fung, MD          Sub-Investigator: Anthony Nichols, MD          Sub-Investigator: Danielle McNeil, MD 收起 <<
NCT02235909 Hypertension Phase 3 Recruiting August 2020 -
NCT00762736 Diabetes Mellitus Phase 2 Completed - -

Azilsartan medoxomil/阿齐沙坦酯 参考文献

[1]Zaiken K, Cheng JW. Azilsartan medoxomil: a new Angiotensin receptor blocker. Clin Ther. 2011 Nov;33(11):1577-89.

[2]Ojima M, Igata H, et al. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther. 2011 Mar;336(3):801-8.

[3]Kusumoto K, Igata H, Ojima M, Tsuboi A, Imanishi M, Yamaguchi F, Sakamoto H, Kuroita T, Kawaguchi N, Nishigaki N, Nagaya H. 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. Eur J Pharmacol. 2011 Nov 1;669(1-3):84-93. doi: 10.1016/j.ejphar.2011.07.014. Epub 2011 Jul 28. PMID: 21816148.

[4]Weber MA, White WB, Sica D, Bakris GL, Cao C, Roberts A, Kupfer S. Effects of combining azilsartan medoxomil with amlodipine in patients with stage 2 hypertension. Blood Press Monit. 2014 Apr;19(2):90-7. doi: 10.1097/MBP.0000000000000027. PMID: 24445723; PMCID: PMC3966914.

[5]Kajiya T, Ho C, Wang J, Vilardi R, Kurtz TW. Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83. doi: 10.1097/HJH.0b013e32834c46fd. PMID: 21986624.

Azilsartan medoxomil/阿齐沙坦酯 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.79mL

1.76mL

0.88mL

17.59mL

3.52mL

1.76mL

Azilsartan medoxomil/阿齐沙坦酯 技术信息

CAS号863031-21-4
分子式C30H24N4O8
分子量 568.53
SMILES Code O=C(C1=C2N(CC3=CC=C(C4=CC=CC=C4C(N5)=NOC5=O)C=C3)C(OCC)=NC2=CC=C1)OCC6=C(C)OC(O6)=O
MDL No. MFCD19443688
别名 TAK-491
运输蓝冰
InChI Key QJFSABGVXDWMIW-UHFFFAOYSA-N
Pubchem ID 135409642
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
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