EPI-743
Based on 1 Customer Validation
EPI-743 (Vatiquinone; α-Tocotrienol quinone; PTC-743; NCT04378075) is a potent cellular oxidative stress protectant, inhibits ferroptosis in cells, which could be used for the study for mitochondrial diseases. EPI-743 is a synthetic analog of vitamin E with oral activity, targets repletion of reduced intracellular glutathione.
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- Pureté : 98.06%
- CAS No.: 1213269-98-7
- Formule: C29H44O3
- Masse moléculaire:440.66
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Stockage:Pure form -20°C, 3 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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HY-100579
Ferrostatin-1Ferroptosis Inhibitor -
HY-N0111
Coenzyme Q10Antioxidant -
HY-134539
IMT1POLRMT Inhibitor -
HY-100410
FCCPOXPHOS Uncoupler -
HY-50856
RuxolitinibJAK1/2 Inhibitor -
HY-12212
OmaveloxoloneNrf2 Activator -
HY-15763
ErastinFerroptosis Inducer -
HY-128895
KL1333NAD+ Modulator -
HY-10254
MirdametinibMEK Inhibitor -
HY-14539
ClozapineAntipsychotic Agent -
HY-134832
Mito-LNDOXPHOS Inhibitor -
HY-N1441
AfzelinFlavonol Glycoside
Activité biologique
Description
IC50 & Target
Mitochondria[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Fibroblast | EC50 |
24 nM
Compound: ATQ3
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Cytoprotectant activity against L-buthionine-(S,R)-sulfoximine-induced cell death in Friedreich ataxia patient fibroblasts assessed as increase of cell viability
Cytoprotectant activity against L-buthionine-(S,R)-sulfoximine-induced cell death in Friedreich ataxia patient fibroblasts assessed as increase of cell viability
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[PMID: 21600768] |
| Fibroblast | EC50 |
30 nM
Compound: ATQ3
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Cytoprotectant activity against L-buthionine-(S,R)-sulfoximine-induced cell death in Leigh syndrome patient fibroblasts assessed as increase of cell viability
Cytoprotectant activity against L-buthionine-(S,R)-sulfoximine-induced cell death in Leigh syndrome patient fibroblasts assessed as increase of cell viability
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[PMID: 21600768] |
In Vitro
Ferroptosis is a form of iron- and lipid-dependent regulated cell death associated with glutathione depletion and production of lipid peroxides by lipoxygenase enzymes.
EPI-743 prevents RSL3-induced ferroptosis in PCH6 patient fibroblasts with mean EC50 potency values of 17.3-21.8 nM[3].
EPI-743 (37, 111, 333 nM; 24 h) exhibits prevention of BODIPY 581/591 C11 lipid oxidation[3].
EPI-743 (0.1 nM-1 mM; 48 h) potently prevents ferroptosis induced by RSL3 (2 μM), FeC (100 μM), BSO (50 μM)[3].
EPI-743 (1 μM, 3 h) is reduced to EPI-743 hydroquinone (EPI-743-HQ) in PCH6 patient fibroblasts, and EPI-743-HQ (0.1-100 μM; 30 min) inhibits human 15-LO enzyme activity with 20% inhibition at 100 μM, and IC50 is 4.4 μM[3].
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:Primary fibroblasts and B-lymphocytes
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Concentration:0-1 mM
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Incubation Time:48 hours
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Result:Inhibited RSL3-mediated ferroptotic cell death in B-lymphocytes in a dose-dependent manner.
Restored viability to levels comparable with untreated cells, indicating complete rescue.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1213269-98-7
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Appearance Liquid (Density: 0.978±0.06 g/cm3)
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Masse moléculaire 440.66
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Formule C29H44O3
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Color Light yellow to yellow
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SMILES
O=C1C(CC[C@](C)(O)CC/C=C(C)/CC/C=C(C)/CC/C=C(C)\C)=C(C)C(C(C)=C1C)=O
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Synonyms
α-Tocotrienol quinone; PTC-743; Vatiquinone; NCT04378075
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (226.93 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: ≥ 2.5 mg/mL (5.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Protocole
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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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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
Pureté et documentation
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Fiche technique (270 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kouga T, et al. Japanese Leigh syndrome case treated with EPI-743. Brain Dev. 2018 Feb;40(2):145-149. Brain Dev. 2018 Feb;40(2):145-149. [Content Brief]
[2]. Avula S, et al. Treatment of Mitochondrial Disorders. Curr Treat Options Neurol. 2014. 16:292.
[3]. Kahn-Kirby AH, et al. Targeting ferroptosis: A novel therapeutic strategy for the treatment of mitochondrial disease-related epilepsy. PLoS One. 2019 Mar 28;14(3):e0214250. [Content Brief]
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 |
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| DMSO | 1 mM | 2.2693 mL | 11.3466 mL | 22.6932 mL | 56.7331 mL |
| 5 mM | 0.4539 mL | 2.2693 mL | 4.5386 mL | 11.3466 mL | |
| 10 mM | 0.2269 mL | 1.1347 mL | 2.2693 mL | 5.6733 mL | |
| 15 mM | 0.1513 mL | 0.7564 mL | 1.5129 mL | 3.7822 mL | |
| 20 mM | 0.1135 mL | 0.5673 mL | 1.1347 mL | 2.8367 mL | |
| 25 mM | 0.0908 mL | 0.4539 mL | 0.9077 mL | 2.2693 mL | |
| 30 mM | 0.0756 mL | 0.3782 mL | 0.7564 mL | 1.8911 mL | |
| 40 mM | 0.0567 mL | 0.2837 mL | 0.5673 mL | 1.4183 mL | |
| 50 mM | 0.0454 mL | 0.2269 mL | 0.4539 mL | 1.1347 mL | |
| 60 mM | 0.0378 mL | 0.1891 mL | 0.3782 mL | 0.9456 mL | |
| 80 mM | 0.0284 mL | 0.1418 mL | 0.2837 mL | 0.7092 mL | |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2269 mL | 0.5673 mL |
EPI-743 Related Classifications
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