Ezetimibe,163222-33-1

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产品名称：Ezetimibe

产品别名：依泽替米贝;依折麦布

英文别名：Ezetimibe

靶点：NPC1L1

CAS：163222-33-1

纯度：>98%

外观：白色或类白色结晶性粉末

保存方法：-20°C

描述：

Ezetimibe (Zetia) is a compound that lowers cholesterol. Ezetimibe (Zetia) acts by decreasing cholesterol absorption in the intestine. Ezetimibe (Zetia) may be used alone, when other cholesterol-lowering medications are not tolerated, or together with statins when statins alone do not control cholesterol. Ezetimibe localises at the brush border of the small intestine, where ezetimibe (Zetia) inhibits the absorption of cholesterol from the intestine. Specifically, ezetimibe (Zetia) appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes.

溶解性：Ethanol ：75 mg/mL (183.2 mM)
DMSO ：75 mg/mL (183.2 mM)

体外研究：

Ezetimibe produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol. Ezetimibe reduces cholesterol transport by 31% in Caco-2 cells, but not retinol transport. Ezetimibe results in a significant decrease in mRNA expression for the surface receptors SR-BI, Niemann-Pick type C1 Like 1 protein (NPC1L1), and ATP-binding cassette transporter, subfamily A (ABCA1) and for the nuclear receptors retinoid acid receptor (RAR)gamma, sterol-regulatory element binding proteins (SREBP)-1 and -2, and liver X receptor (LXR)beta as assessed by real-time PCR analysis in Caco-2 cells.

体内研究：Ezetimibe reduces plasma cholesterol levels from 964 to 374 mg/dL, from 726 to 231 mg/dL, and from 516 to 178 mg/dL in the western, low-fat, and cholesterol-free diet mice, respectively. Ezetimibe reduces aortic atherosclerotic lesion surface area from 20.2% to 4.1% in the western diet group and from 24.1% to 7.0% in the low-fat cholesterol diet mice. Ezetimibe reduces carotid artery atherosclerotic lesion cross-sectional area by 97% in the western and low-fat cholesterol groups and by 91% in the cholesterol-free mice. Ezetimibe inhibits cholesterol absorption, reduces plasma cholesterol, increases high density lipoprotein levels, and inhibits the progression of atherosclerosis under western, low-fat, and cholesterol-free dietary conditions in apoE-/- mice. Ezetimibe potently inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. Ezetimibe eliminates exocrine pancreatic function from the intestine while maintaining bile flow, is established in the rat. Ezetimibe reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg.

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