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阿齐沙坦

阿齐沙坦用途

Azilsartan(TAK-536)是特异且高活性的血管紧张素Ⅱ1型受体拮抗剂,IC50为2.6 nM。

阿齐沙坦名称

[ CAS 号 ]:
147403-03-0

[ 中文名 ]:
阿齐沙坦

[ 英文名 ]:
Azilsartan

[中文别名 ]:

克林霉素

[英文别名 ]:

TAK 536
Azilsartan
UNII-F9NUX55P23

阿齐沙坦生物活性

[ 描述 ]:

Azilsartan(TAK-536)是特异且高活性的血管紧张素Ⅱ1型受体拮抗剂,IC50为2.6 nM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管紧张素受体

研究领域 >> 心血管疾病

[参考文献]

[1]. Ojima M, Igata H, Tanaka M, 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]. Weltman R, Brands CM, Corral E, Assessment of the environmental fate and effects of azilsartan, a selective antagonist of angiotensin II type 1. Chemosphere. 2012 Jun;87(11):1323-9.

[3]. Pierini D, Anderson KV. Azilsartan medoxomil/chlorthalidone: a new fixed-dose combination antihypertensive. Ann Pharmacother. 2013 May;47(5):694-703.

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

[相关活性小分子]

阿齐沙坦物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 分子式 ]:
C₂₅H₂₀N₄O₅

[ 分子量 ]:
456.450

[ 精确质量 ]:
456.143372

[ PSA ]:
123.24000

[ LogP ]:
4.21

[ 外观性状 ]:
white to beige

[ 折射率 ]:
1.695

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: soluble15mg/mL (clear solution)

阿齐沙坦MSDS

阿齐沙坦安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

阿齐沙坦合成路线

阿齐沙坦文献

Liquid chromatography/tandem mass spectrometry study of forced degradation of azilsartan medoxomil potassium.

Rapid Commun. Mass Spectrom. 29 , 1437-47, (2015)

Azilsartan medoxomil potassium (AZM) is a new antihypertensive drug introduced in the year 2011. The presence of degradation products not only affects the quality, but also the safety aspects of the d...

Olmesartan blocks advanced glycation end products-induced vcam-1 gene expression in mesangial cells by restoring Angiotensin-converting enzyme 2 level.

Horm. Metab. Res. 46(6) , 379-83, (2014)

Advanced glycation end products (AGEs) and their receptor (RAGE) system are involved in diabetic nephropathy. Angiotensin-converting enzyme 2 (ACE 2) plays a protective role against cardiovascular and...

Azilsartan Improves Salt Sensitivity by Modulating the Proximal Tubular Na+-H+ Exchanger-3 in Mice.

PLoS ONE 11 , e0147786, (2016)

A potent angiotensin II type-1 receptor blocker, azilsartan, has been reported to reduce blood pressure more effectively than candesartan. Interestingly, azilsartan can also restore the circadian rhyt...

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阿齐沙坦

阿齐沙坦用途

阿齐沙坦名称

阿齐沙坦生物活性

阿齐沙坦物理化学性质

阿齐沙坦MSDS

详细MSDS(安全技术说明书)

阿齐沙坦安全信息

阿齐沙坦合成路线

详细合成路线

阿齐沙坦文献

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