1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-hydroxy-propyl]-4-(4-hydroxyphenyl)-azetidin-2-one EZETIMIBE ZETIA
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Product information
Ezetimibe Basic information |
Cholesterol-lowering drugs |
Product Name: | Ezetimibe |
Synonyms: | 1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-hydroxy-propyl]-4-(4-hydroxyphenyl)-azetidin-2-one;EZETIMIBE;ZETIA;Ezitimibe∬EzetimibeC24H21F2N03;(3R,4S)-1-(4-Fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-2-azetidinone, Sch-58235;1-(4-Flurophenyl)-(3R)-3-(4-flurophenyl)-(3S)-hydroxypropyl-(4S)-(4-hydroxyphenyl)-2-azetidinone;Ezetimide |
CAS: | 163222-33-1 |
MF: | C24H21F2NO3 |
MW: | 409.43 |
EINECS: | |
Product Categories: | All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Final material;API;Isotope;CEDAX;Cardiovascular APIs;Ezetimibe |
Mol File: | 163222-33-1.mol |
Ezetimibe Chemical Properties |
mp | 164-166°C |
storage temp. | -20 C Freezer |
CAS DataBase Reference | 163222-33-1(CAS DataBase Reference) |
Ezetimibe Usage And Synthesis |
Cholesterol-lowering drugs |
Ezetimibe,jointly developed by Schering-Plough and Merck companies ,is the first selective cholesterol absorption inhibitor, the product is first approved by the US FDA listed as selective cholesterol absorption inhibitor class of drugs. Trade name is"EZETROL". Ezetimibe is a new selective cholesterol absorption inhibitor, it is also the first selective inhibitor of intestinal cholesterol absorption, and its mechanism of action is different from other lipid-lowering agents (such as: statins, bile acid sequestrants, phenoxy acid derivative thereof cattle and plant sterol ester compound), the product ,through binding with the intestinal brush border membrane vesicle membrane protein (relative molecular mass 145X103), inhibits intestinal absorption of cholesterol which is from diet and transported to the intestine via the bile tract , reduces serum and liver cholesterol. Different from acid chelating agent ,ezetimibe does not affect cholesterol esters, other steroids (such as bezoar acid), triglycerides and fat-soluble vitamin absorption. Its pharmacological effects have nothing to do with acetyl coenzyme A- cholesterol acetyltransferase (ACAT) inhibiting and LDL receptors (scavenger receptor) expression . After being absorbed in the liver , ezetimibe combined with glucuronic acid by enterohepatic circulation,is almost specifically targeting to the small intestine mucosa. It can be used alone or in combination with HMG-CoA reductase inhibitors (statins) jointly applied to the treatment of primary (heterozygous familial and non-familial) hypercholesterolemia, homozygous familial hypercholesterolemia (HoFH) homozygous sitosterol hyperlipidemia (hyperlipidemia or phytosterols). The above information is edited by the chemicalbook of Tian Ye. |
Chemical Properties | White Solid |
Usage | An antihyperlipoproteinemic. A Cholesterol absorption inhibitor |
Usage | antibacterial |
Usage | A cholesterol transport inhibitor that binds to NPC1L1 |
Usage | For use 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. |
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