Ezetimibe ketone
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.97%
- CAS No.: 191330-56-0
- Formula: C24H19F2NO3
- Molecular Weight:407.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-100523
ML385Nrf2 Inhibitor -
HY-N1913
DanshensuNrf2/HO-1 Activator -
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AstilbinTNF Receptor Inhibitor -
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4-Hydroxyphenylacetic acidEndogenous Metabolite -
HY-120912
Gingerenone ANrf2-Gpx4 Activator -
HY-110258
ML334NRF2 Activator -
HY-N0826
CorynolineAChE Inhibitor -
HY-122550
ArtemisiteneNrf2 Activator -
HY-111126
K67Keap1/S349-p-p62 Interaction Inhibitor -
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OmaveloxoloneNrf2 Activator -
HY-133114R
Ezetimibe ketone (Standard)Analytical Standard -
HY-Z0548
Methyl 3,4-dihydroxybenzoate
Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:rat renal tubular epithelial NRK-52E cells
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Concentration:5-50 μM
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Incubation Time:24 h
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Result:Showed no cytotoxic effects on NRK-52E cells.
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Cell Line:rat renal tubular epithelial NRK-52E cells (treated with 300 μM H₂O₂)
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Concentration:5-50 μM (concurrent with H₂O₂); 25 μM (6 h before, concurrent with, or 6 h after H₂O₂)
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Incubation Time:24 h (H₂O₂ treatment duration)
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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.
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Cell Line:rat renal tubular epithelial NRK-52E cells (treated with 300 μM H₂O₂)
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Concentration:25 μM
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Incubation Time:6 h before, concurrent with, or 6 h after H₂O₂ exposure; 24 h (H₂O₂ treatment duration)
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 7 weeks old, 300 ± 10 g, renal ischemia-reperfusion injury model)[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 4 consecutive days (last dose 30 min before surgery)
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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.
Chemical Information
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CAS No. 191330-56-0
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Appearance Solid
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Molecular Weight 407.41
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Formula C24H19F2NO3
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Color White to off-white
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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
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Synonyms
EZM-K
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (280 KB)
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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)
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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 |
Ezetimibe ketone Related Classifications
HY-133114 Related Classifications
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