Ezetimibe
Catalog #
27749-2
$170
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Description
Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it 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.
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Synonyms
ezetimibe; Zetia; (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
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Product Data Gallery
Product Info
Storage and Usage
Citations
Target(s)
Cholesterol absorption
Formula
C24H21F2NO3
MW
409.4 Da
Solubility
Soluble in DMSO
Biological Activity
Ezetimibe glucuronide inhibits bromosulfophthalein uptake in all OATP-transfected cells with an IC50 ranging from 140 to 260 nM.
CAS Registry #
163222-33-1
Background
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.
References
Garcia-Calvo M, et al. Proc Natl Acad Sci U S A. 2005 Jun 7;102(23):8132-7.
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