| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MDH2-IN-2 (compound 28i) inhibited the activity of recombinant human MDH1 enzyme with an IC50 value of 25.3 μM[1]. MDH2-IN-2 (1 μM; 3 days) significantly downregulated the mRNA levels of multiple SASP factors in MRC-5 cells and reduced the expression level of p53 protein and the proportion of SA-β-gal positive cells in replicative senescent MRC-5 cells[1]. MDH2-IN-2 (1 μM) significantly reduced the proportion of SA-β-gal positive cells in mitomycin C-induced senescent NRK-52E cells[1]. MDH2-IN-2 (1 μM; 5 days) significantly reduced the expression level of p16 protein and the proportion of SA-β-gal positive cells in replicative senescent MEF cells[1]. MDH2-IN-2 (1 μM; 5-60 min) undergoes rapid metabolic turnover in human and mouse liver microsomes, with corresponding T1/2 values of 1.15 min and 1.10 min, respectively [1].
|
|---|---|
| ln Vivo |
MDH2-IN-2 (100 μM; incorporated into NGM medium; continuous exposure) can extend the average lifespan of wild-type Caenorhabditis elegans by 15.49% and improve a number of indicators related to healthy lifespan[1]. MDH2-IN-2 (0-50 mg/kg; gavage; once daily; for 3 weeks) can significantly inhibit multiple SASP factors in male C57BL/6J mice with premature aging induced by doxorubicin[1]. MDH2-IN-2 (5-10 mg/kg; gavage; once daily; for 3 months) can reverse age-related serum biochemical abnormalities in naturally aging male C57BL/6J mice, inhibit the production of SASP factors, reduce the expression of renal aging markers, and improve renal histological morphology[1].
|
| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: MRC-5 cells Tested Concentrations: 1 μM Incubation Duration: 3 days Experimental Results: Significantly downregulated the mRNA expression of aging-associated secretory phenotype (SASP) factors IL-1α, IL-1β, IL-8, CXCL-1, MMP-1 and MMP-3. Western Blot Analysis [1] Cell Types: Replicated senescent human embryonic lung fibroblasts (MRC-5, passage 32) Tested Concentrations: 1 μM Incubation Duration: 3 days Experimental Results: Significantly reduced the expression level of p53 protein, a key senescence-related cell cycle regulator. Western Blot analysis [1] Cell Types: Replicated senescent mouse embryonic fibroblasts (MEF, 7th generation) Tested Concentrations: 1 μM Incubation Duration: 5 days Experimental Results: Significantly reduced the protein expression level of p16, a key senescence-related cyclin-dependent kinase inhibitor. |
| Animal Protocol |
Animal/Disease Models:Wild-type N2[1]
Doses: 100 μM Route of Administration: Incorporated into NGM medium; continuous exposure Experimental Results: Compared with the control group, the average lifespan was extended by 15.49%. Compared with the control group, the oviposition capacity was significantly improved. Compared with the control group, the pharyngeal pumping frequency increased. Compared with the control group, the body bending frequency remained unchanged. Animal/Disease Models:C57BL/6J (male, 8 weeks old, doxorubicin-induced premature aging)[1] Doses: 10 mg/kg; 20 mg/kg; 50 mg/kg Route of Administration: Gavage; once daily; 3 weeks Experimental Results: Serum levels of SASP factors (including IL-1β, IL-6, CXCL-1, TNF-α, MMP-1 and MMP-2) were significantly reduced compared to male mice treated with doxorubicin alone. Animal/Disease Models:C57BL/6J (male, 21 months old, naturally aged) [1] Doses: 5 mg/kg; 10 mg/kg Route of Administration: Gavage; once daily for 3 months Experimental Results: Significantly reduced age-related elevations in serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), blood urea nitrogen (BUN), and uric acid (UA), bringing them to levels comparable to those in young control mice. Significantly reduced serum levels of aging-associated secretory phenotype (SASP) factors, including IL-6, IL-1β, MMP-1, MMP-2, CXCL-1, GDF-15, and TNF-α. Downregulated the expression of aging markers p53, p21, and p16 in renal tissue. Significantly improved age-related glomerular atrophy, inflammatory infiltration, and renal collagen fiber accumulation. |
| References |
| Molecular Formula |
C31H40N2O4S
|
|---|---|
| Molecular Weight |
536.73
|
| CAS # |
3047410-41-0
|
| Appearance |
Typically exists as solids at room temperature
|
| 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
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8631 mL | 9.3157 mL | 18.6313 mL | |
| 5 mM | 0.3726 mL | 1.8631 mL | 3.7263 mL | |
| 10 mM | 0.1863 mL | 0.9316 mL | 1.8631 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
