Azilsartan medoxomil

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Chemical Structure| 863031-21-4 同义名 : TAK-491
CAS号 : 863031-21-4
货号 : A325842
分子式 : C30H24N4O8
纯度 : 95%
分子量 : 568.53
MDL号 : MFCD19443688
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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].
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 - -
实验方案
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
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.