Home Metabolism LDL modulator Ezetimibe (SCH-58235)

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Ezetimibe (SCH-58235) LDL modulator

Cat.No.S1655

Ezetimibe (SCH-58235) is a potent, selective, cholesterol absorption inhibitor that is used to lower cholesterol.
Ezetimibe (SCH-58235) LDL modulator Chemical Structure

Chemical Structure

Molecular Weight: 409.4

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Quality Control

Batch: Purity: 99.91%
99.91

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (200.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 409.4 Formula

C24H21F2NO3

 Storage (From the date of receipt)
CAS No. 163222-33-1 Download SDF Storage of Stock Solutions

Synonyms SCH-58235 SMILES C1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O

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Mechanism of Action

Targets/IC50/Ki
NPC1L1
In vitro
Ezetimibe (SCH-58235) produces a significant reduction in total cholesterol, LDL cholesterol, and triglycerides as well as a small but significant increase in HDL cholesterol. This compound reduces cholesterol transport by 31% in Caco-2 cells, but not retinol transport. It 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 (SCH-58235) 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. It 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. This compound 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. It 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. It eliminates exocrine pancreatic function from the intestine while maintaining bile flow, as established in the rat. The compound reduces plasma cholesterol and hepatic cholesterol accumulation in cholesterol-fed hamsters with an ED(50) of 0.04 mg /kg.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16801428/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11564660/
  • [6] https://pubmed.ncbi.nlm.nih.gov/17587760/

Applications

Methods Biomarkers Images PMID
Western blot PCSK9 / LDLR / SREBP2 / HNF1-a LC3B-I / LC3B-II / Nuclear TFEB p-AMPK / AMPK
S1655-WB3
25889684

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-08-07)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06722521 RECRUITING
Primary Prevention; Vascular Calcification
Asan Medical Center
 2025-07-09 PHASE4
NCT07524101 RECRUITING
Renal Insufficiency; Atherosclerosis; Dyslipidemia; Hypercholesterolemia; Cardiovascular Diseases
Yonsei University
 2026-05-28
NCT05579626 ENROLLING_BY_INVITATION
Pre Diabetes; ASCVD
Seung-Whan Lee, M.D., Ph.D.
 2023-03-14 PHASE4
NCT06649240 RECRUITING
Ischemic Stroke; Small Vessel Cerebrovascular Disease; Cholesterol, LDL; Secondary Prevention; Cardiovascular Diseases
Seoul National University Hospital
 2024-10-04
NCT07359105 RECRUITING
Dyslipidemia Associated With Type II Diabetes Mellitus
Sin Gon Kim
 2026-03-09
NCT07799779 NOT_YET_RECRUITING
Acute Coronary Syndromes (ACS)
Seoul National University Bundang Hospital
 2026-09 PHASE4

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Frequently Asked Questions

Question 1:
I am planning to deliver it per orally and wonder proper vehicle for this compound and effective dose level for lowering intestinal cholesterol absorption.

Answer:
It 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 compound in DMSO clearly first. Then add PEG 300 and Tween 80, after mixed homogeneously, then dilute with water.