For research use only.

Catalog No.S1655 Synonyms: SCH-58235

11 publications

Ezetimibe  Chemical Structure

Molecular Weight(MW): 409.4

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

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 130 In stock
USD 70 In stock
USD 97 In stock
USD 137 In stock
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Selleck's Ezetimibe has been cited by 11 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.

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Choose Selective LDL Inhibitors

Biological Activity

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

Methods Test Index PMID
Western blot
p-AMPK / AMPK ; 

PubMed: 28933629     

Representative immunoblot analysis of primary hepatocytes treated with 20 or 50 μM ezetimibe for 16 h, pre-treated with ezetimibe for 2 h followed by 2 mM oleate (OA), or treated with 2 mM metformin (Met) for 16 h. n = 3–5.

LC3B-I / LC3B-II / Nuclear TFEB ; 

PubMed: 28933629     

Representative immunoblots of primary hepatocytes treated with 50 μM ezetimibe at 0, 2, 8, and 16 hours. n = 3–5.

PCSK9 / LDLR / SREBP2 / HNF1-a ; 

PubMed: 25889684     

Western blot showed (A): in ezetimibe group, the expression of PSCK9, LDLR and SREBP2 increased significantly in all organs,while the expression of HNF-1α increased markedly only in liver.

28933629 25889684
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]


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(Data is from Selleck tests instead of citations):
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.

Chemical Information

Molecular Weight 409.4


CAS No. 163222-33-1
Storage powder
in solvent
Synonyms SCH-58235
Smiles OC(CCC1C(N(C1=O)C2=CC=C(F)C=C2)C3=CC=C(O)C=C3)C4=CC=C(F)C=C4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04197453 Recruiting -- ASCVD Amgen|Duke Clinical Research Institute December 6 2019 --
NCT04322266 Completed Drug: HCP1701|Drug: HCP1306|Drug: HGP0904|Drug: HGP0608 Healthy Hanmi Pharmaceutical Company Limited December 21 2018 Phase 1
NCT03434613 Completed Drug: Rosuvastatin|Drug: Rosuvastatin/ezetimibe combination Nonalcoholic Fatty Liver Disease|Dyslipidemias Yonsei University May 14 2018 Phase 4

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.

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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