Art. -Nr.: HY-17376

Ezetimibe

Name: Ezetimibe
Brand: MedChemExpress
SKU: HY-17376
Price: 39.00 USD
Availability: InStock
Rating: 5 (16 reviews)

(Synonyms: SCH 58235)

16 Cited Publications

Kundenbewertung

Based on 16 publication(s) in Google Scholar

Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.

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Reinheit : 99.88%
CAS. Nr.: 163222-33-1
Formel: C₂₄H₂₁F₂NO₃
Molecular Weight:409.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Ezetimibe Chemical Structure

CAS. Nr.: 163222-33-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.

IC₅₀ & Target

NPC1L1, Nrf2^[1]

In Vitro

Ezetimibe (Eze) acts as a potent Nrf2 activator without causing cytotoxicity. Ezetimibe enhances transactivation of Nrf2, as revealed by a luciferase reporter assay. Ezetimibe also upregulates Nrf2 target genes, including GSTA1, heme oxygenase-1 (HO-1) and Nqo-1 in Hepa1c1c7 and MEF cells. Ezetimibe upregulates Nrf2 target genes in Nrf2+/+ MEF cells, whereas this induction is totally blocked in Nrf2-/- MEF cells. Taken together, Ezetimibe acts as a novel Nrf2 inducer in a ROS-independent manner^[1]. Human huh7 hepatocytes are pretreated with Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h) to induce hepatic steatosis. Ezetimibe treatment significantly attenuates PA-increased triglycerides (TG) levels, which is consistent with our animal study. PA treatment resulted in an approximately 20% decrease in mRNA expression of ATG5, ATG6, and ATG7, which had been increased by Ezetimibe treatment. In addition, Ezetimibe treatment significantly increased the PA-induced reduction in LC3 protein abundance^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

Administration of Ezetimibe (Eze) reduces the liver weights of mice fed the methionine- and choline-deficient (MCD) diet. This is consistent with the beneficial effects of Ezetimibe on hepatic steatosis. Liver histology shows pronounced multiple macrovesicular fat droplets in mice on the MCD diet, but Ezetimibe treatment markedly decreases the number and size of those droplets. Furthermore, hepatic fibrosis in mice fed the MCD diet is significantly attenuated by Ezetimibe^[1]. Blood and liver lipid levels including TG, free fatty acids (FFA), and total cholesterol (TC) are significantly decreased in Ezetimibe-treated OLETF rats. Moreover, OLETF rats show higher serum levels of glucose, insulin, HOMA-IR, TG, FFA, and TC than LETF animals, which are significantly reduced by Ezetimibe. In addition, histological analysis indicated that OLETF control rats showed larger lipid droplets in hepatocytes than age-matched LETO controls, which are attenuated by administration of Ezetimibe^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 163222-33-1
Appearance Solid
Molecular Weight 409.43
Formel C₂₄H₂₁F₂NO₃
Color White to off-white
SMILES

O=C1N(C2=CC=C(F)C=C2)[C@H](C3=CC=C(O)C=C3)[C@H]1CC[C@@H](C4=CC=C(F)C=C4)O
Synonyms

SCH 58235
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (16)

All Bio/Physico-chemical AssayCell Proliferation/Viability AssayFlow CytometryWBIn Vivo Efficacy Study

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Journal Impact Factor

Signal Transduct Target Ther

Maternal cholesterol deficiency predisposes congenital heart defects risk. [Abstract]

2025 Nov 12;10(1):366. PMID: 41219186

Ezetimibe purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 12;10(1):366. [Abstract]

At embryonic day 12.5 (E12.5), maternal serum cholesterol levels in the Ezetimibe (Eze) (0.005% (w/w))- and Ator-treated groups were reduced by an average of 16.4% and 23.5%, respectively, compared with those in the control group, primarily through a decrease in low-density lipoprotein (LDL) cholesterol levels with no significant effect on high-density lipoprotein (HDL) cholesterol levels.
Cell

A two-front nutrient supply environment fuels small intestinal physiology through differential regulation of nutrient absorption and host defense. [Abstract]

2024 Oct 31;187(22):6251-6271.e20. PMID: 39427662
J Exp Clin Cancer Res

SCP2-mediated cholesterol membrane trafficking promotes the growth of pituitary adenomas via Hedgehog signaling activation. [Abstract]

2019 Sep 13;38(1):404. PMID: 31519191

Ezetimibe purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Sep 13;38(1):404. [Abstract]

Ezetimibe (30 mg/kg, i.p.) inhibited tumor growth in vivo.
Food Res Int

Hydroxypropyl-β-cyclodextrin as a co-delivery vehicle for synergistically enhancing fucoxanthin oral bioavailability through dual regulation of SR-B1 and ABCB1 transporters. [Abstract]

2026 Mar 31:228:118352. PMID: 41703824
J Chem Inf Model

Development of Machine Learning Models and the Discovery of a New Antiviral Compound against Yellow Fever Virus. [Abstract]

2021 Aug 23;61(8):3804-3813. PMID: 34286575
Nutrients

2026 Jan;18(9):1389.
Front Cell Dev Biol

Structural and Functional Characterization of Fibronectin in Extracellular Vesicles From Hepatocytes. [Abstract]

2021 Mar 18:9:640667. PMID: 33816490
Orphanet J Rare Dis

High content drug screening for Fanconi anemia therapeutics. [Abstract]

2020 Jun 30;15(1):170. PMID: 32605631
Brain Res

Ezetimibe mitigates microglial activation in Parkinson's disease via TLR4/JNK pathway inhibition: evidence from network pharmacology and experimental validation. [Abstract]

2026 Feb 15:1873:150116. PMID: 41419122
J Diabetes Complications

Ezetimibe attenuates diabetic retinopathy via NRF2-mediated suppression of inflammation and oxidative stress. [Abstract]

2025 Dec 13;40(2):109250. PMID: 41411956
FEBS Open Bio

Ezetimibe inhibits the migration and invasion of triple-negative breast cancer cells by targeting TGFβ2 and EMT. [Abstract]

2024 May;14(5):831-842. PMID: 38531630
Virology

Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]

2023 Aug:585:205-214. PMID: 37384967
In Silico Research in Biomedicine 2025 Nov 6;1:100116
SSRN

2025 Jul 8.
Orebro University

2024.
Heliyon

Ezetimibe inhibits triple-negative breast cancer proliferation and promotes cell cycle arrest by targeting the PDGFR/AKT pathway. [Abstract]

2023 Oct 29;9(11):e21343. PMID: 38027998

Ezetimibe purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Oct 29;9(11):e21343. [Abstract]

Viability of MDA-MB-231 and 4T1 cells treated with different concentrations of Ezetimibe (0, 1, 5, 10, 15, 20, 40, 60, 80, 100 μmol/L) for 48 h was detected using the CCK-8 assay.

Ezetimibe purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Oct 29;9(11):e21343. [Abstract]

Flow cytometry analysis was conducted to examine cell cycle distribution of MDA-MB-231 and 4T1 cells treated with different concentrations of Ezetimibe (0, 20, 40 μmol/L) for 48 h.

Ezetimibe purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Oct 29;9(11):e21343. [Abstract]

Western blotting was performed to determine the expression levels of Ki67, CDK2, CDK4, and CyclinD1 proteins in MDA-MB-231 and 4T1 cells treated with different concentrations of Ezetimibe (0, 20, 40 μmol/L) for 48 h.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 200 mg/mL (488.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4424 mL

12.2121 mL

24.4242 mL

5 mM

0.4885 mL

2.4424 mL

4.8848 mL

10 mM

0.2442 mL

1.2212 mL

2.4424 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 5 mg/mL (12.21 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Korean - KR (761 KB)
- Portuguese - PT (761 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lee DH, et al. Ezetimibe, an NPC1L1 inhibitor, is a potent Nrf2 activator that protects mice from diet-induced nonalcoholic steatohepatitis. Free Radic Biol Med. 2016 Sep 12;99:520-532. [Content Brief]

[2]. Chang E, et al. Ezetimibe improves hepatic steatosis in relation to autophagy in obese and diabetic rats. World J Gastroenterol. 2015 Jul 7;21(25):7754-63. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4424 mL	12.2121 mL	24.4242 mL	61.0605 mL
	5 mM	0.4885 mL	2.4424 mL	4.8848 mL	12.2121 mL
	10 mM	0.2442 mL	1.2212 mL	2.4424 mL	6.1060 mL
	15 mM	0.1628 mL	0.8141 mL	1.6283 mL	4.0707 mL
	20 mM	0.1221 mL	0.6106 mL	1.2212 mL	3.0530 mL
	25 mM	0.0977 mL	0.4885 mL	0.9770 mL	2.4424 mL
	30 mM	0.0814 mL	0.4071 mL	0.8141 mL	2.0353 mL
	40 mM	0.0611 mL	0.3053 mL	0.6106 mL	1.5265 mL
	50 mM	0.0488 mL	0.2442 mL	0.4885 mL	1.2212 mL
	60 mM	0.0407 mL	0.2035 mL	0.4071 mL	1.0177 mL
	80 mM	0.0305 mL	0.1527 mL	0.3053 mL	0.7633 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6106 mL

Bioz

Keywords

Ezetimibe

16 Cited Publications

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Ezetimibe

Publications Citing Use of MedChemExpress (MCE) Ezetimibe