2. NF-κB Autophagy
  3. Keap1-Nrf2 Autophagy
  4. Ezetimibe

Ezetimibe  (Synonyms: SCH 58235)

Cat. No.: HY-17376 Purity: 99.72%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Ezetimibe Chemical Structure

Ezetimibe Chemical Structure

CAS No. : 163222-33-1

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10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 67 In-stock
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10 mg USD 61 In-stock
50 mg USD 88 In-stock
100 mg USD 110 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Ezetimibe:

Ezetimibe Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

Ezetimibe Related Antibodies
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
Molecular Weight

409.43

Formula

C24H21F2NO3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4424 mL 12.2121 mL 24.4242 mL
5 mM 0.4885 mL 2.4424 mL 4.8848 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.72%

COA (255 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

GST-p62 is prepared from Escherichia coli and 0.5 μg of the purified GST-p62 protein is used for in vitro AMPK phosphorylation assay. Phosphorylation of p62 protein by AMPK is determined by non-radioisotope method using γS-ATP. AMPK complex is immuno-purified from the HEK293 cells, to which either myc-AMPKα1 wild-type (WT) or myc-AMPKα1 kinase-dead mutant (KD, D157A) is transfected with Flag-AMPKβ1 and HA-AMPKγ1. AMPK complex is added into the reaction mixture containing 20 mM HEPES, pH7.4, 1 mM EGTA, 0.4 mM EDTA, 5 mM MgCl2, 0.05 mM DTT, 0.5 μg GST-p62, 0.2 mM AMP, and 1 mM ATPγS. Reaction is carried out at 37°C for 30 min, and then terminated by adding 20 mM EDTA. To detect γS-labeled p62 protein, the reaction product is alkylated with 2.5 mM PNBM for 2 h at room temperature and analyzed the products by western blotting using anti-thiophosphate antibody[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

Huh7 human hepatocytes are cultured in high glucose DMEM containing 10% FBS, 100 units/mL penicillin and 100 μg/mL streptomycin at 37°C in a 95% air/5% CO2 atmosphere. Hepatocytes are treated with or without Ezetimibe (10 μM, 1 h) and incubated with palmitic acid (PA, 0.5 mM, 24 h)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][2]

Mice[1]
Ten-week-old C57BL/6J male mice are used. These animals are randomly assigned to one of three groups (7-10 mice in each group): normal chow diet; MCD diet, vehicle-treated; or MCD diet, Ezetimibe -treated. The mice had free access to diet and water, with temperature maintained at 23±2°C, humidity of 60%±10%, and 12-h light/dark cycles. In the MCD diet with Ezetimibe group, Ezetimibe 10 mg/kg is given once daily by oral gavage for 4 weeks. The chow and MCD diet with vehicle groups received the same volume of phosphate buffered saline orally for 4 weeks. Body weight is measured once a week over the course of the treatment period. After 4 weeks, the mice are anesthetized and killed; blood is collected via heart puncture. Tissues are harvested and either snap-frozen in liquid nitrogen and stored at −70°C or fixed in formalin and embedded in paraffin.
Rats[2]
Male OLETF (n=11) and age-matched LETO rats (n=3) are used, and experiments are conducted in a specific pathogen-free facility with a 12 h light/dark cycle. The OLETF rat is a model that represents late-onset hyperglycemia and exhibits a chronic disease course, mild obesity and clinical onset of diabetes mellitus. Animals have unrestricted access to water and food. At 12 wk of age, rats are randomized and treated with either PBS or Ezetimibe (10 mg/kg per day) via a stomach gavage for 20 wk. At the end of the study, the rats are fasted overnight and anesthetized with intraperitoneal Zoletil/Rompun. Blood is collected from the abdominal aorta, and liver tissues are dissected, immediately frozen in liquid nitrogen, and stored at -80°C until further analysis.

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

Complete Stock Solution Preparation Table

* 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.

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
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Ezetimibe Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ezetimibe163222-33-1SCH 58235SCH58235SCH-58235Keap1-Nrf2AutophagyInhibitorinhibitorinhibit

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