| 应用 |
A cholesterol transport inhibitor that binds to NPC1L1 |
| 产品介绍 |
Ezetimibe has been reported to be a cholesterol transport inhibitor. Mechanistic studies show that this compound directly affects Niemann-Pick C1-like 1 (NPC1L1) and prevents it from incorporating into clathrin-coated vesicles. NPC1L1 is a polytopic transmembrane protein that facilitates absorption of cholesterol via clathrin/AP2-mediated endocytosis. By binding to NPC1L1, ezetimibe prevents endocytosis of this protein therefore blocking cholesterol transfer across membranes. Ezetimibe is used clinically to lower plasma cholesterol levels. |
| 备注 |
Ezetimibe (Zetia) is a compound that lowers cholesterol. |
| 生化机理 |
Ezetimibe inhibits intestinal cholesterol absorption by preventing cholesterol uptake by Niemann-Pick C1 Like 1 (NPC1L1) protein that was found critical for the intestinal absorption of cholesterol. Ezetimibe selectvely blocks cholesterol absorption without inhibiting pancreatic lipolytic enzyme activities in the intestinal lumen. Ezetimibe is a non statin drug that reduces intestinal cholesterol absorption. In addition, it also has an ability to reduce the risk of cardiovascular events in patients who had had an acute coronary syndrome and whose low-density lipoprotein (LDL) cholesterol values were within guideline recommendations. |
| 别名 |
Zetia;Ezetrol;依泽替米贝; (3R,4S)-1-(4-氟苯基)-3-[(S)-3-(4-氟苯基)-3-羟基丙基]-4-(4-羟基苯基)-2-氮杂环丁酮;依折麦布
;Zetia;Ezetrol |
