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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.
Biological Activity: Ezetimibe glucuronide inhibits bromosulfophthalein uptake in all OATP-transfected cells with an IC50 ranging from 140 to 260 nM.
CAS Number: 163222-33-1
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.
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: Cholesterol absorption
Biosafety Level: Not applicable (BSL-1)
References: Garcia-Calvo M, et al. Proc Natl Acad Sci U S A. 2005 Jun 7;102(23):8132-7.
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