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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 血管紧张素受体 / Azilsartan

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

货号：A217890 同义名： TAK-536

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

Azilsartan 化学结构 CAS号：147403-03-0
Azilsartan 化学结构
CAS号：147403-03-0
Azilsartan 3D分子结构
CAS号：147403-03-0
Azilsartan 化学结构 CAS号：147403-03-0
Azilsartan 3D分子结构 CAS号：147403-03-0
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Azilsartan 纯度/质量文件 产品仅供科研

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Azilsartan 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].

Azilsartan 动物研究

Dose Mice: 1 mg/kg - 10 mg/kg[3] (p.o.) Rat: 10 mg/kg[4] (p.o.), 0.3 mg/kg - 3 mg/kg[5] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[6] Dogs[6] Monkeys[6]
Dose 1 mg/kg (p.o.)
0.2 mg/kg (i.v.) 		1 mg/kg (p.o.)
0.2 mg/kg (i.v.) 		3 mg/kg (p.o., fasted)
0.2 mg/kg (i.v., fasted)
Administration p.o.
i.v. 		p.o.
i.v. 		p.o.
i.v.
F 14.6% (p.o.) 24.3% (p.o.) 13.6% (p.o.)
AUC0→24h 7.26 μg·h/ml (p.o.)
9.97 μg·h/ml (i.v.) 		1.18 μg·h/ml (p.o.)
0.97 μg·h/ml (i.v.) 		6.71 μg·h/ml (p.o.)
3.36 μg·h/ml (i.v.)
T1/2 5.2 h (p.o.) 2.9 h (p.o.) 1.4 h (p.o.)
1.6 h (i.v.)
Tmax 1.7 h (p.o.) 0.8 h (p.o.) 1.7 h (p.o.)
Cmax 0.901 μg/ml (p.o.) 0.247 μg/ml (p.o.) 0.264 μg/ml (p.o.)
3.637 μg/ml (i.v.)

Azilsartan 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 - -

Azilsartan 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.

Azilsartan 实验方案

计算器
存储液制备 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

Azilsartan 技术信息

CAS号147403-03-0
分子式C25H20N4O5
分子量 456.45
别名 TAK-536
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
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

Tags: Azilsartan | TAK-536 | Angiotensin Receptor | AmBeed-信号通路专用抑制剂 | Azilsartan 纯度/质量文件 | Azilsartan 生物活性 | Azilsartan 动物研究 | Azilsartan 临床数据 | Azilsartan 参考文献 | Azilsartan 实验方案 | Azilsartan 技术信息

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