产品名称

阿齐沙坦(Azilsartan)

一般描述

Azilsartan is an angiotensin II receptor blocker (ARB) used in the therapy of hypertension.

别 称

1-[[2′-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)   [1,1′-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid; 阿奇沙坦; TAK-536

纯 度

≥99.0%(HPLC)

CAS NO.

147403-03-0

分子式

C²⁵H²⁰N⁴O⁵

分子量

456.45

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Azilsartan medoxomil is a newly approved angiotensin receptor blocker (ARB) reported to lower 24 hr blood pressure more effectively than maximally recommended doses of older ARBs. Although azilsartan is considered to be an unusually potent angiotensin II type 1 (AT1) receptor antagonist, little is known about the potential pleiotropic effects of this molecule. /The purpose of this study was to investigate/ pleiotropic features of azilsartan in cell-based assay systems independent of its effects on blood pressure. In cultured 3T3-L1 preadipocytes, azilsartan enhanced adipogenesis and exerted greater effects than valsartan on of genes encoding peroxisome proliferator-activated receptor-a (PPARa), PPARd, leptin, adipsin, and adiponectin. The effects of azilsartan on adipocyte differentiation and gene were observed at concentrations of azilsartan that did not classically stimulate PPAR activity in cell-based transactivation assays. Azilsartan also potently inhibited vascular cell proliferation in the absence of exogenously supplemented angiotensin II. In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 umol/L, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 umol/L.Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors. In addition, azilsartan, but not valsartan, blocked angiotensin II-induced activation of mitogen-activated protein kinase in vascular smooth muscle cells 4-8 hr after washout of drug from the incubation media. These findings suggest that azilsartan can function as a pleiotropic ARB with potentially beneficial effects on cellular mechanisms of cardiometabolic disease through actions that could involve more than just blockade of AT1 receptors and/or reduction in blood pressure.

l  包装与存储

包 装

250mg; 1g

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov