MDH2-IN-2
Based on 1 Customer Validation
MDH2-IN-2 is an orally active MDH2 inhibitor with an IC50 of 5.9 μM. MDH2-IN-2 reduces the levels of senescence markers and senescence-associated secretory phenotype (SASP) factors in mammalian cell models. MDH2-IN-2 extends the lifespan and improves the healthspan of Caenorhabditis elegans. MDH2-IN-2 alleviates tissue senescence in aged mice, inhibits SASP factors, and restores liver and kidney functions. MDH2-IN-2 is applicable for senescence-related research.
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- Pureté: 99.91%
- CAS No.: 3047410-41-0
- Formule: C31H40N2O4S
- Masse moléculaire:536.73
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
MDH2-IN-2 (Compound 28i) inhibits the activity of recombinant human MDH1 enzyme, with an IC50 value of 25.3 μM[1].
MDH2-IN-2 (1 μM; 3 days) significantly downregulates the mRNA levels of various SASP factors in MRC-5 cells, and reduces the expression level of p53 protein and the proportion of SA-β-gal-positive cells in replicatively senescent MRC-5 cells[1].
MDH2-IN-2 (1 μM) significantly reduces the proportion of SA-β-gal-positive NRK-52E cells that undergo senescence induced by Mitomycin C (HY-13316)[1].
MDH2-IN-2 (1 μM; 5 days) significantly reduces the expression level of p16 protein and the proportion of SA-β-gal positive cells in replicative senescent MEFs[1].
MDH2-IN-2 (1 μM; 5-60 minutes) undergoes rapid metabolic turnover in both human and mouse liver microsomes, with corresponding T1/2 values of 1.15 min and 1.10 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MRC-5 cells
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Concentration:1 μM
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Incubation Time:3 days
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Result:Significantly downregulated mRNA expression of senescence-associated secretory phenotype (SASP) factors IL-1α, IL-1β, IL-8, CXCL-1, MMP-1, and MMP-3.
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Cell Line:Replicatively senescent human embryonic lung fibroblasts (MRC-5, passage 32)
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Concentration:1 μM
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Incubation Time:3 days
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Result:Significantly reduced the protein expression level of p53, a key senescence-associated cell cycle regulator.
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Cell Line:Replicatively senescent mouse embryonic fibroblasts (MEFs, passage 7)
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Concentration:1 μM
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Incubation Time:5 days
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Result:Significantly reduced the protein expression level of p16, a key senescence-associated cyclin-dependent kinase inhibitor.
MDH2-IN-2 (0-50 mg/kg; i.g.; once daily; 3 weeks) significantly inhibits multiple SASP factors in premature senescent male C57BL/6J mice induced by Doxorubicin (HY-15142A)[1].
MDH2-IN-2 (5-10 mg/kg; i.g.; once daily; 3 months) reverses age-related serum biochemical abnormalities, inhibits the production of SASP factors, reduces the expression of renal senescence markers, and improves renal histological morphology in naturally aged male C57BL/6J mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type N2[1]
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Dosage:100 μM
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Administration:incorporation into NGM plates; continuous exposure
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Result:Extended mean lifespan by 15.49% compared to controls.
Significantly improved egg-laying capacity compared to controls.
Increased pharyngeal pumping rate compared to controls.
Maintained body bend frequency relative to controls.
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Animal Model:C57BL/6J (male, 8 weeks old, doxorubicin-induced premature aging)[1]
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Dosage:10 mg/kg; 20 mg/kg; 50 mg/kg
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Administration:i.g.; once daily; 3 weeks
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Result:Significantly reduced serum levels of SASP factors including IL-1β, IL-6, CXCL-1, TNF-α, MMP-1, and MMP-2 compared to Dox-only treated male mice.
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Animal Model:C57BL/6J (male, 21 months old, naturally aged)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.g.; once daily; 3 months
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Result:Significantly reduced age-related increases in serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), blood urea nitrogen (BUN), and uric acid (UA) to levels comparable to young control mice.
Markedly reduced serum levels of SASP factors including IL-6, IL-1β, MMP-1, MMP-2, CXCL-1, GDF-15, and TNF-α.
Downregulated renal tissue expression of senescence markers p53, p21, and p16.
Significantly ameliorated age-related glomerular atrophy, inflammatory infiltration, and collagen fiber accumulation in the kidney.
Chemical Information
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CAS No. 3047410-41-0
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Appearance Solid
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Masse moléculaire 536.73
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Formule C31H40N2O4S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C=C1)CCNC(C2=CC=CC(OCC3CCCC3)=C2)=O)(NC45C[C@@H]6C[C@H](C5)C[C@@H](C6)C4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 100 mg/mL (186.31 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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 (4.66 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.66 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 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (sealed storage, away from moisture). 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 | 1.8631 mL | 9.3157 mL | 18.6313 mL | 46.5784 mL |
| 5 mM | 0.3726 mL | 1.8631 mL | 3.7263 mL | 9.3157 mL | |
| 10 mM | 0.1863 mL | 0.9316 mL | 1.8631 mL | 4.6578 mL | |
| 15 mM | 0.1242 mL | 0.6210 mL | 1.2421 mL | 3.1052 mL | |
| 20 mM | 0.0932 mL | 0.4658 mL | 0.9316 mL | 2.3289 mL | |
| 25 mM | 0.0745 mL | 0.3726 mL | 0.7453 mL | 1.8631 mL | |
| 30 mM | 0.0621 mL | 0.3105 mL | 0.6210 mL | 1.5526 mL | |
| 40 mM | 0.0466 mL | 0.2329 mL | 0.4658 mL | 1.1645 mL | |
| 50 mM | 0.0373 mL | 0.1863 mL | 0.3726 mL | 0.9316 mL | |
| 60 mM | 0.0311 mL | 0.1553 mL | 0.3105 mL | 0.7763 mL | |
| 80 mM | 0.0233 mL | 0.1164 mL | 0.2329 mL | 0.5822 mL | |
| 100 mM | 0.0186 mL | 0.0932 mL | 0.1863 mL | 0.4658 mL |
MDH2-IN-2 Related Classifications
HY-181604 Related Classifications
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