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Synonyms:
MDH2-IN-2
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | MDH2-IN-2 is an orally active MDH2 inhibitor with an IC50 of 5.9 μM. It reduces the levels of senescence markers and senescence-associated secretory phenotype (SASP) factors in mammalian cell models. Additionally, MDH2-IN-2 extends the lifespan and enhances the health span of Caenorhabditis elegans. In aged mice, MDH2-IN-2 alleviates tissue aging, inhibits SASP factors, and restores liver and kidney function. MDH2-IN-2 is applicable in aging-related research. |
| In vitro | MDH2-IN-2 (Compound 28i) inhibits the activity of recombinant human MDH1 enzyme with an IC50 of 25.3 μM. At 1 μM for 3 days, MDH2-IN-2 significantly downregulates mRNA levels of multiple SASP factors in MRC-5 cells, decreases p53 protein expression, and reduces the proportion of SA-β-gal-positive cells in replicative senescent MRC-5 cells. In NRK-52E cells, MDH2-IN-2 at 1 μM significantly lowers the proportion of SA-β-gal-positive cells induced by Mitomycin C. Additionally, at 1 μM over 5 days, it significantly decreases p16 protein expression and the proportion of SA-β-gal-positive cells in replicative senescent MEFs. Rapid metabolic turnover of MDH2-IN-2 is observed in both human and mouse liver microsomes, with half-lives of 1.15 min and 1.10 min, respectively, at concentrations ranging from 5 to 60 minutes. |
| In vivo | MDH2-IN-2, when used at a concentration of 100 μM incorporated into NGM plates for continuous exposure, can extend the average lifespan of wild-type Caenorhabditis elegans by 15.49% and improve various health-related indicators. Additionally, MDH2-IN-2 administered at 0-50 mg/kg (intraperitoneal, once daily for 3 weeks) significantly inhibits multiple SASP factors in doxorubicin-induced progeroid male C57BL/6J mice. In another study, daily intraperitoneal administration of MDH2-IN-2 at doses of 5-10 mg/kg for 3 months in naturally aging male C57BL/6J mice was found to reverse age-related serum biochemical abnormalities, suppress the production of SASP factors, reduce the expression of renal aging markers, and improve renal histological morphology. |
| Molecular Weight | 536.73 |
| Formula | C31H40N2O4S |
| Cas No. | 3047410-41-0 |
| Smiles | O=C(NCCC1=CC=C(C=C1)S(=O)(=O)NC23CC4CC(CC(C4)C2)C3)C=5C=CC=C(OCC6CCCC6)C5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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