GPX4 activator 2
Based on 1 Customer Validation
GPX4 activator 2 is a GPX4 activator with a Ka value of 0.426 μM for human GPX4. GPX4 activator 2 reduces lipid hydroperoxide levels, prevents lipid peroxide accumulation, and inhibits ferroptosis. GPX4 activator 2 rescues cell death induced by Erastin (HY-15763). GPX4 activator 2 exerts cardioprotective effects in a mouse model of doxorubicin (HY-15142A)-induced myocardial injury.
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- Pureté : 99.23%
- CAS No.: 950365-31-8
- Formule: C20H26N6O2S
- Masse moléculaire:414.52
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
GPX4 0.426 μM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HT-1080 | EC50 |
7.8 μM
Compound: C3
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Reversal of erastin induced cell death in human HT-1080 cells assessed as cell viability preincubated for 1 hr followed by erastin addition and measured after 24 hrs by CCK8 method
Reversal of erastin induced cell death in human HT-1080 cells assessed as cell viability preincubated for 1 hr followed by erastin addition and measured after 24 hrs by CCK8 method
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[PMID: 39096818] |
In Vitro
GPX4 activator 2 (compound C3) rescues Erastin (HY-15763)-induced ferroptosis in HT1080 cells with an EC50 of 7.80 μM (24 h)[1].
GPX4 activator 2 (10 μM; 2 h) prevents erastin-induced lipid peroxide accumulation in HT1080 cells[1].
GPX4 activator 2 binds to purified human GPX4 protein at regions covering peptides 18-29, 68-87, and 92-102[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with Myocardial injury (8-week-old male)[1]
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Dosage:10 mg/kg; 25 mg/kg
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Administration:i.p.; single injection 24h pre-DOX
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Result:Reduced serum MDA levels to ~3.2 μM, cardiac MDA levels to ~240 μmol/mg, and cardiac AST levels to ~105 U/L at 10 mg/kg compared to DOX model group (serum MDA ~4.1 μM, cardiac MDA ~380 μmol/mg, cardiac AST ~130 U/L).
Reduced serum MDA levels to ~2.2 μM, cardiac MDA levels to ~180 μmol/mg, and cardiac AST levels to ~85 U/L at 25 mg/kg.
Reduced nuclear pyknosis, vacuolar degeneration, and inflammatory infiltration at 10 mg/kg compared to Doxorubicin model.
Showed nearly normal myocardial cell arrangement, no significant vacuolar degeneration or fibrosis, and minimal inflammatory infiltration or nuclear damage at 25 mg/kg.
Chemical Information
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CAS No. 950365-31-8
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Appearance Solid
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Masse moléculaire 414.52
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Formule C20H26N6O2S
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Color White to off-white
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SMILES
CN(CC1)CCN1C2=NN=C(S2)N3C=CC=C3CNC4=CC=C(OC)C=C4OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (241.24 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 6.25 mg/mL (15.08 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (15.08 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.4124 mL | 12.0621 mL | 24.1243 mL | 60.3107 mL |
| 5 mM | 0.4825 mL | 2.4124 mL | 4.8249 mL | 12.0621 mL | |
| 10 mM | 0.2412 mL | 1.2062 mL | 2.4124 mL | 6.0311 mL | |
| 15 mM | 0.1608 mL | 0.8041 mL | 1.6083 mL | 4.0207 mL | |
| 20 mM | 0.1206 mL | 0.6031 mL | 1.2062 mL | 3.0155 mL | |
| 25 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4124 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8041 mL | 2.0104 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6031 mL | 1.5078 mL | |
| 50 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 60 mM | 0.0402 mL | 0.2010 mL | 0.4021 mL | 1.0052 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7539 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2412 mL | 0.6031 mL |
GPX4 activator 2 Related Classifications
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