Ezetimibe Inhibitor CAS No. 163222-33-1

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KI0822	Ezetimibe	50 mg	$155.2

Chemical Characteristic

Product Name	Ezetimibe
Synonyms	Zetia, Ezetrol, SCH 488128
CAS No.	163222-33-1
Molecular Weight	409.43
Formula	C₂₄H₂₁F₂NO₃
Chemical Structure

Biological activities

Ezetimibe is an inhibitor of the intestinal cholesterol uptake protein Niemann-Pick C1 like 1. Ezetimibe glucuronide inhibits bromosulfophthalein uptake in all OATP-transfected cells with an IC50 ranging from 140 to 260 nM.^[1] Ezetimibe acts by decreasing cholesterol absorption in the intestine. Ezetimibe decreases cholesterol levels. Ezetimibe causes a small but statistically significant effect on plasma levels of ciclosporin. ^[2] Ezetimibe reduces cholesterol transport by 31%, but not retinol transport.^[3] Ezetimibe inhibits sterol uptake increased by NPC1L1 overexpression.^[4] Ezetimibe significantly decreases total and LDL cholesterol concentrations by -14.5% and -22.0%, respectively.^[5] In sr-b1(-/-)/apoE(-/-) mice, ezetimibe significantly reduces aortic sinus plaque, coronary arterial occlusion, myocardial fibrosis and cardiomegaly by 57%, 68%, 57% and 12%, respectively.^[6] Ezetimibe inhibits expression of acid sphingomyelinase in liver and intestine.^[7]

Protocols

In vitro: Ezetimibe is dissolved in DMSO.^[7]

References

[1] Oswald S, et al. Disposition of ezetimibe is influenced by polymorphisms of the hepatic uptake carrier OATP1B1. Pharmacogenet Genomics. 2008 Jul;18(7):559-568. [2] Kosoglou T, et al. Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005, 44(5): 467-494. 閵嗏偓閵嗏偓 [3] During A, et al. Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. J Nutr. 2005, 135(10): 2305-2312. 閵嗏偓閵嗏偓 [4] Yamanashi Y, Niemann-Pick C1-like 1 overexpression facilitates ezetimibe-sensitive cholesterol and beta-sitosterol uptake in CaCo-2 cells. J Pharmacol Exp Ther. 2007, 320(2): 559-564. 閵嗏偓閵嗏偓 [5] Tremblay AJ, et al. Effect of ezetimibe on the in vivo kinetics of apoB-48 and apoB-100 in men with primary hypercholesterolemia. Arterioscler Thromb Vasc Biol. 2006, 26(5): 1101-1106. 閵嗏偓閵嗏偓 [6] Davis HR Jr, et al. Effects of ezetimibe on atherosclerosis in preclinical models. Atherosclerosis. 2011, 215(2): 266-278. 閵嗏偓閵嗏偓 [7] Cheng Y, et al. Ezetimibe inhibits expression of acid sphingomyelinase in liver and intestine. Lipids. 2009, 44(10): 897-906. 閵嗏偓閵嗏偓

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