Catalog No.S1655 Synonyms: SCH-58235
Molecular Weight(MW): 409.4
Ezetimibe is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.
Cited by 6 Publications
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
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|Description||Ezetimibe is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.|
Ezetimibe produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol.  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. 
|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.  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.  Ezetimibe reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg. |
-  Clader JW, et al. J Med Chem, 2004, 47(1), 1-9.
-  During A, et al. J Nutr, 2005, 135(10), 2305-2312.
-  Davis HR Jr, et al. Arterioscler Thromb Vasc Biol, 2001, 21(12), 2032-2038.
|In vitro||DMSO||81 mg/mL (197.85 mM)|
|Ethanol||81 mg/mL (197.85 mM)|
|In vivo||Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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.
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Frequently Asked Questions
I am planning to deliver Ezetimibe per orally and wonder proper vehicle for Ezetimbie and effective dose level for lowering intestinal cholesterol absorption.
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.