产品名称

坎地沙坦酯(Candesartan Cilexetil)

一般描述

Candesartan Cilexetil(坎地沙坦酯) is a synthetic, benzimidazole-derived angiotensin II receptor antagonist prodrug with antihypertensive activity.

别 称

2-ethoxy-1-[[2′ -(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-Benzimidazole-7-carboxylic   acid 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester; TCV 116, TCY 116

纯 度

≥98.0%(HPLC)

CAS NO.

145040-37-5

分子式

C³³H³⁴N⁶O⁶

分子量

610.66

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

Slightly soluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Candesartan Cilexetil is a synthetic, benzimidazole-derived angiotensin II receptor antagonist prodrug with antihypertensive activity. After hydrolysis of candesartan cilexetil to candesartan during gastrointestinal absorption, candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. In addition, antagonism of AT1 in the adrenal gland inhibits angiotensin II-stimulated aldosterone synthesis and secretion by the adrenal cortex; sodium and water excretion increase, followed by a reduction in plasma volume and blood pressure.

The prodrug candesartan cilexetil undergoes rapid and complete ester hydrolysis in the intestinal wall to form the active drug, candesartan. Elimination of candesartan is primarily as unchanged drug in the urine and, by the biliary route, in the feces. Minor hepatic metabolism of candesartan (<20%) occurs by O-deethylation via cytochrome P450 2C9 to form an inactive metabolite. Candesartan undergoes N-glucuronidation in the tetrazole ring by uridine   diphosphate glucuronosyltransferase 1A3 (UGT1A3). O-glucuronidation may also occur. 75% of candesartan is excreted as unchanged drug in urine and feces.

Candesartan selectively blocks the binding of angiotensin II to AT1 in many tissues including vascular smooth muscle and the adrenal glands. This inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in an overall decrease in blood pressure. Candesartan is greater than 10,000 times more selective for AT1 than AT2. Inhibition of aldosterone secretion may increase sodium and water excretion while decreasing potassium excretion.

l  包装与存储

包 装

250mg; 1g; 5g

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