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

Ezetimibe ketone is an orall active Nrf2 activator and ROS inhibitor. Ezetimibe ketone attenuates H2O2-induced reactive oxygen species production and reduces H2O2-induced apoptosis in renal tubular epithelial cells. Ezetimibe ketone suppresses renal tubular injury and inflammation.

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Ezetimibe ketone

Ezetimibe ketone Chemical Structure

CAS No. : 191330-56-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Ezetimibe ketone:

Ezetimibe ketone Related Antibodies

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  • Purity & Documentation

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Description

Ezetimibe ketone is an orall active Nrf2 activator and ROS inhibitor. Ezetimibe ketone attenuates H2O2-induced reactive oxygen species production and reduces H2O2-induced apoptosis in renal tubular epithelial cells. Ezetimibe ketone suppresses renal tubular injury and inflammation[1].

IC50 & Target

NPC1L1, Nrf2[1]
In Vitro

Ezetimibe ketone (5-50 μM; 24 h) does not induce cytotoxicity in rat renal tubular epithelial NRK-52E cells[1].
Ezetimibe ketone (5-50 μM; 24 h, concurrent with H2O2) reduces H2O2-induced apoptosis in rat renal tubular epithelial NRK-52E cells; ezetimibe ketone (25 μM; administered before, during, or after H2O2 exposure) reduces H2O2-induced apoptosis and ROS production, with maximal inhibition when added simultaneously with H2O2[1].
Ezetimibe ketone (5-50 μM; 24 h, concurrent with H2O2) preserves mitochondrial membrane potential in H2O2-treated rat renal tubular epithelial NRK-52E cells; ezetimibe ketone (25 μM; administered before, during, or after H2O2 exposure) preserves ΔΨm, with maximal preservation when added simultaneously with H2O2[1].
Ezetimibe ketone (5-50 μM; 24 h, concurrent with H2O2) inhibits H2O2-induced Caspase-3/7 activation in rat renal tubular epithelial NRK-52E cells; ezetimibe ketone (25 μM; administered before, during, or after H2O2 exposure) inhibits Caspase-3/7 activation, with maximal inhibition when added simultaneously with H2O2[1].
Ezetimibe ketone (25 μM; administered before, during, or after H2O2 exposure for 24 h) activates the Nrf2/HO-1 signaling pathway by increasing nuclear and cytoplasmic Nrf2 and HO-1 protein levels in H2O2-treated rat renal tubular epithelial NRK-52E cells[1].
The protective effects of ezetimibe ketone (25 μM; concurrent with 300 μM H2O2 for 24 h, with simultaneous 10 μM SnPP or 5 μM ML385 co-treatment) against H2O2-induced injury in rat renal tubular epithelial NRK-52E cells are mediated via the Nrf2/HO-1 signaling pathway, as co-treatment with Nrf2 or HO-1 inhibitors reverses ezetimibe ketone-induced pathway activation and protective effects[1].

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

Ezetimibe ketone Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: rat renal tubular epithelial NRK-52E cells
Concentration: 5-50 μM
Incubation Time: 24 h
Result: Showed no cytotoxic effects on NRK-52E cells.

Apoptosis Analysis[1]

Cell Line: rat renal tubular epithelial NRK-52E cells (treated with 300 μM H₂O₂)
Concentration: 5-50 μM (concurrent with H₂O₂); 25 μM (6 h before, concurrent with, or 6 h after H₂O₂)
Incubation Time: 24 h (H₂O₂ treatment duration)
Result: Significantly reduced H₂O₂-induced apoptosis in NRK-52E cells. Reduced H₂O₂-induced apoptosis and reactive oxygen species production, with the strongest effect observed when added simultaneously with H₂O₂.

Western Blot Analysis[1]

Cell Line: rat renal tubular epithelial NRK-52E cells (treated with 300 μM H₂O₂)
Concentration: 25 μM
Incubation Time: 6 h before, concurrent with, or 6 h after H₂O₂ exposure; 24 h (H₂O₂ treatment duration)
Result: Significantly increased nuclear Nrf2 and HO-1 protein levels compared to H₂O₂ treatment alone. Increased cytoplasmic Nrf2 and HO-1 protein levels relative to H₂O₂ treatment alone.
In Vivo

Ezetimibe ketone (10 mg/kg; p.o.; daily; 4 consecutive days) activates the Nrf2/HO-1 signaling pathway, suppresses renal tubular injury and inflammation, improves renal function, and protects against renal ischemia-reperfusion injury in Sprague-Dawley rats[1].

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

Animal Model: Sprague-Dawley (male, 7 weeks old, 300 ± 10 g, renal ischemia-reperfusion injury model)[1]
Dosage: 10 mg/kg
Administration: p.o.; daily; 4 consecutive days (last dose 30 min before surgery)
Result: Significantly reduced serum blood urea nitrogen (BUN) and serum creatinine (SCr) levels compared to untreated RIRI rats.\nSignificantly decreased renal tissue mRNA expression levels of proinflammatory cytokines TNF-α and IL-1β.\nReduced renal tubular injury including tubular necrosis, cast formation, and tubular dilation.\nDecreased renal cell apoptosis (measured via TUNEL staining).\nReduced renal immune cell infiltration (measured via F4/80 immunohistochemistry).\nSignificantly increased nuclear and total protein expression levels of Nrf2 and HO-1 in kidney tissues.
Molecular Weight

407.41

Formula

C24H19F2NO3
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]1CCC(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 : 100 mg/mL (245.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4545 mL 12.2726 mL 24.5453 mL
5 mM 0.4909 mL 2.4545 mL 4.9091 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.

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.25 mg/mL (3.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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% (20% SBE-β-CD in Saline)

    Solubility: 1.25 mg/mL (3.07 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.25 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 (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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: 99.97%

SDS (761 KB)

COA (250 KB) HNMR (286 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.4545 mL 12.2726 mL 24.5453 mL 61.3632 mL
5 mM 0.4909 mL 2.4545 mL 4.9091 mL 12.2726 mL
10 mM 0.2455 mL 1.2273 mL 2.4545 mL 6.1363 mL
15 mM 0.1636 mL 0.8182 mL 1.6364 mL 4.0909 mL
20 mM 0.1227 mL 0.6136 mL 1.2273 mL 3.0682 mL
25 mM 0.0982 mL 0.4909 mL 0.9818 mL 2.4545 mL
30 mM 0.0818 mL 0.4091 mL 0.8182 mL 2.0454 mL
40 mM 0.0614 mL 0.3068 mL 0.6136 mL 1.5341 mL
50 mM 0.0491 mL 0.2455 mL 0.4909 mL 1.2273 mL
60 mM 0.0409 mL 0.2045 mL 0.4091 mL 1.0227 mL
80 mM 0.0307 mL 0.1534 mL 0.3068 mL 0.7670 mL
100 mM 0.0245 mL 0.1227 mL 0.2455 mL 0.6136 mL
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Ezetimibe ketone Related Classifications

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  • 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:

Ezetimibe ketone191330-56-0EZM-KKeap1-Nrf2AutophagyNrf2/HO-1 signaling pathwayrenal tubular epithelial cellsNrf2Caspase-3/7ROSapoptosisrenal ischemia-reperfusion injuryNRK-52E cellsHO-1Sprague-Dawley ratsInhibitorinhibitorinhibit

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