Azilsartan

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Chemical Structure| 147403-03-0 同义名 : TAK-536
CAS号 : 147403-03-0
货号 : A217890
分子式 : C25H20N4O5
纯度 : 98%
分子量 : 456.45
MDL号 : MFCD20278186
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(54.77 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

生物活性
靶点

  • AT1 receptor

    AT1 receptor, IC50:2.6 nM
描述 The numerous effects of Angiotensin II (AII), including its roles in vasoconstriction, secretion of aldosterone and vasopressin, cellular proliferation, and hypertrophy are dominantly mediated through the activation of the angiotensin type 1 (AT1) receptor, a member of the superfamily of G protein-coupled receptors. Azilsartan (AZL) is an AT1 receptor antagonist with IC50 of 2.6 nM. Pretreatment of AZL for 90 min inhibited the specific binding of 125I-Sar1-Ile8-AII to human AT1 receptors expressed in CHO cells in a concentration-related manner with an IC50 of 2.6 nM, indicating a high affinity for AT1 receptors. A potent inhibitory effect of AZL at AT1 receptors was maintained even 5 h after washout with an IC50 value of 7.4 nM. Pretreatment of intact COS-7 cells expressing human AT1 receptor with AZL for 2 h inhibited the accumulation of IP1 with IC50 value of 9.2 nM. Pretreatment with 0.1, 0.3, or 1 nM AZL for 30 min inhibited AII-induced aortic contraction in a concentration-related manner [7].
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 -
NCT00362115 Hypertension Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL
参考文献

[1]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.

[2]Iwai M, Chen R, et al. TAK-536, a new AT1 receptor blocker, improves glucose intolerance and adipocyte differentiation. Am J Hypertens. 2007 May;20(5):579-86.

[3]Iwanami J, Mogi M, et al. Role of angiotensin-converting enzyme 2/angiotensin-(1-7)/Mas axis in the hypotensive effect of azilsartan. Hypertens Res. 2014 Jul;37(7):616-20.

[4]A9641 Novel Angiotensin II Receptor Blocker Azilsartan protects myocardium from ischemic reperfusion injury in experimental rats through Peroxisome Proliferator–Activated Receptor- γ Activation

[5]Takai S, Jin D, et al. Significance of the vascular concentration of angiotensin II-receptor blockers on the mechanism of lowering blood pressure in spontaneously hypertensive rats. J Pharmacol Sci. 2013;123(4):371-9. Epub 2013 Nov 29.

[6]TAK-536

[7]Ojima M, Igata H, Tanaka M, Sakamoto H, Kuroita T, Kohara Y, Kubo K, Fuse H, Imura Y, Kusumoto K, Nagaya H. 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. doi: 10.1124/jpet.110.176636. Epub 2010 Dec 1. PMID: 21123673.