Ezetimibe (SCH-58235)

For research use only.

Catalog No.S1655

13 publications

Ezetimibe (SCH-58235) Chemical Structure

CAS No. 163222-33-1

Ezetimibe (SCH-58235) is a potent, selective, cholesterol absorption inhibitor, used to lower cholesterol.

Selleck's Ezetimibe (SCH-58235) has been cited by 13 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 (SCH-58235) 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 (SCH-58235) purchased from Selleck.

Purity & Quality Control

Choose Selective LDL Inhibitors

Biological Activity

Description Ezetimibe (SCH-58235) 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]

Assay
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]

Protocol

Solubility (25°C)

In vitro DMSO 81 mg/mL (197.85 mM)
Water Insoluble
Ethanol '81 mg/mL
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.
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
in solvent
Synonyms N/A
Smiles C1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04929249 Recruiting Drug: Inclisiran Atherosclerotic Cardiovascular Disease Novartis Pharmaceuticals|Novartis June 25 2021 Phase 3
NCT04770389 Completed Drug: Obicetrapib 5mg|Drug: Ezetimibe 10mg|Other: Placebo Dyslipidemias|High Cholesterol|Hypercholesterolemia NewAmsterdam Pharma February 23 2021 Phase 2
NCT04762407 Active not recruiting Drug: HGP1910|Drug: HGP1909|Drug: HCP1903 Healthy Hanmi Pharmaceutical Company Limited November 20 2020 Phase 1
NCT04643093 Active not recruiting Drug: Pitavastatin|Drug: Ezetimibe|Drug: 1PC111 Primary Hypercholesterolemia|Mixed Dyslipidemias Orient Pharma Co. Ltd. August 1 2020 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