产品名称

依折麦布(EzetiMibe)

一般描述

Ezetimibe(依折麦布) is an azetidinone derivative and a cholesterol absorption inhibitor with  lipid-lowering activity.

别 称

(3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one;  依泽替米贝;Zetia;  Ezetrol; Ezedoc; Ezetimib

纯 度

≥99%(HPLC)

CAS NO.

163222-33-1

分子式

C²⁴H²¹F²NO³

分子量

409.433

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至类白色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol  and related phytosterols. Ezetimibe, administered alone is indicated as  adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and  Apo B in patients with primary (heterozygous familial and non-familial)  hypercholesterolemia. It is also used in combination therapy with HMG-CoA reductase inhibitors. Ezetimibe has a mechanism of action that differs from  those of other classes of cholesterol-reducing compounds (HMG-CoA reductase  inhibitors, bile acid sequestrants, fibric acid derivatives, and plant stanols). Ezetimibe does not inhibit cholesterol synthesis in the liver, or increase bile acid excretion but instead localizes and appears to act at the brush border of the small intestine and inhibits the absorption of  cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism  is complementary to that of HMG-CoA reductase inhibitors.

Ezetimibe is an azetidinone derivative and a cholesterol absorption inhibitor with lipid-lowering activity. Ezetimibe  appears to interact physically with cholesterol transporters at the brush  border of the small intestine and inhibits the intestinal absorption of  cholesterol and related phytosterols. As a result, ezetimibe causes a decrease in the level of blood cholesterol or an increase in the clearance of  cholesterol from the bloodstream. Overall, the following effects observed are a reduction of hepatic cholesterol stores and a reduction of total cholesterol, LDL cholesterol, and other triglycerides in the blood.

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