Ezetimibe

Catalog No.S1655 Synonyms: SCH-58235

Ezetimibe  Chemical Structure

Molecular Weight(MW): 409.4

Ezetimibe is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 970 In stock
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2 Customer Reviews

  • Caco-2 cells grown in transwell inserts were transfected with scrambled siRNA, or siRNA specific for CCK1R, CCK2R, or both CCK1 and CCK2R and then incubated with 0.002 uCi of [3H]cholesterol micelles in the apical compartment and with culture medium alone (Control) or 10 nm [Thr28,Nle31]CCK with or without 50 uM ezetimibe (EZ) in the basolateral compartment. Absorbed [3H]cholesterol was determined by radioactivity counting of the basolateral medium. Values represent the mean ± S.E. (error bars) of 4-5 independent experiments. *, p < 0.05 versus control; †, p < 0.05 versus cells treated with CCK alone; ‡, p < 0.05 versus cells transfected with scrambled siRNA alone; $, p < 0.05 versus cells treated with scrambled siRNA and CCK.

    J Biol Chem 2014 289(19), 12989-99. Ezetimibe purchased from Selleck.

    Effect of bile duct ligation, proglumide or ezetimibe on cholecystokinin-elevated plasma cholesterol. LDLR-/- mice were subjected to bile duct ligation (BDL), or intravenous injection of 150 mg/kg proglumide, or were gavage-fed with 5 mg/kg ezetimibe. At 30 min after bile duct ligation, or the administration of proglumide or ezetimibe, mice were intravenously injected with 50 ng/kg of cholecystokinin (CCK) or an equal volume of PBS (control) Blood samples were collected at 2 h after CCK or vehicle injection. Plasma cholesterol was measured with a colorimetric assay. Differences among samples obtained from mice before (control) and after treatment with CCK alone, CCK+BDL, CCK+proglumide or CCK+ezetimibe were analyzed by two-way ANOVA followed by Tukey post-hoc tests. Values represent the mean ± SEM of six independent experiments. *P<0.05 compared to control, and †P<0.05 compared to CCK treatment alone.

    PLoS One 2012 7(12), e51011. Ezetimibe purchased from Selleck.

Purity & Quality Control

Choose Selective LDL Inhibitors

Biological Activity

Description Ezetimibe is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.
Targets
NPC1L1 [6]
In vitro

Ezetimibe produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol. [1] Ezetimibe reduces cholesterol transport by 31% in Caco-2 cells, but not retinol transport. Ezetimibe results in a significant decrease in mRNA expression for the surface receptors SR-BI, Niemann-Pick type C1 Like 1 protein (NPC1L1), and ATP-binding cassette transporter, subfamily A (ABCA1) and for the nuclear receptors retinoid acid receptor (RAR)gamma, sterol-regulatory element binding proteins (SREBP)-1 and -2, and liver X receptor (LXR)beta as assessed by real-time PCR analysis in Caco-2 cells. [2]

In vivo Ezetimibe reduces plasma cholesterol levels from 964 to 374 mg/dL, from 726 to 231 mg/dL, and from 516 to 178 mg/dL in the western, low-fat, and cholesterol-free diet mice, respectively. Ezetimibe reduces aortic atherosclerotic lesion surface area from 20.2% to 4.1% in the western diet group and from 24.1% to 7.0% in the low-fat cholesterol diet mice. Ezetimibe reduces carotid artery atherosclerotic lesion cross-sectional area by 97% in the western and low-fat cholesterol groups and by 91% in the cholesterol-free mice. Ezetimibe inhibits cholesterol absorption, reduces plasma cholesterol, increases high density lipoprotein levels, and inhibits the progression of atherosclerosis under western, low-fat, and cholesterol-free dietary conditions in apoE-/- mice. [3] Ezetimibe potently inhibits the transport of cholesterol across the intestinal wall, thereby reducing plasma cholesterol in preclinical animal models of hypercholesterolemia. Ezetimibe eliminates exocrine pancreatic function from the intestine while maintaining bile flow, is established in the rat. [4] Ezetimibe reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg. [5]

Protocol

Solubility (25°C)

In vitro DMSO 81 mg/mL (197.85 mM)
Ethanol 81 mg/mL (197.85 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 409.4
Formula

C24H21F2NO3

CAS No. 163222-33-1
Storage powder
Synonyms SCH-58235

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03051100 Recruiting Hypercholesterolemia Esperion Therapeutics January 2017 Phase 2
NCT02971033 Not yet recruiting Chronic Hepatitis C VA Office of Research and Development January 2017 Phase 2
NCT03001076 Recruiting Hypercholesterolemia|Atherosclerosis|Statin Adverse Reaction Esperion Therapeutics December 2016 Phase 3
NCT02984982 Recruiting Hypercholesterolemia|Acute Coronary Syndrome Sanofi|Regeneron Pharmaceuticals November 2016 Phase 4
NCT02890992 Recruiting Hypercholesterolaemia Sanofi|Regeneron Pharmaceuticals September 2016 Phase 2
NCT02715726 Recruiting Hypercholesterolemia Sanofi|Regeneron Pharmaceuticals July 2016 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    I am planning to deliver Ezetimibe per orally and wonder proper vehicle for Ezetimbie and effective dose level for lowering intestinal cholesterol absorption.

  • Answer:

    S1655 Ezetimibe can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml clearly. If you are going to use this vehicle, please dissolve the drug in DMSO clearly first. Then add PEG 300 and Tween 80, after mixed homogeneously, then dilute with water.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID