| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
HD202A (compound 26) (0.1–1 μM) dose-dependently inhibited MNK-mediated eIF4E phosphorylation in A549 cells [1]. HD202A (1 μM) reduced lipid droplet accumulation and downregulated Plin2 expression in differentiated 3T3-L1 adipocytes without causing cytotoxicity [1]. HD202A (1 μM; 24–36 h) reduced PA-induced lipid accumulation in HepG2 cells, restored lipid homeostasis, and improved mitochondrial function; at a concentration of 25 μM, it inhibited HepG2 cell proliferation [1].
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|---|---|
| ln Vivo |
HD202A (compound 26) (12.5-50 mg/kg; orally; once daily; for 11 weeks) reduced MASLD in male C57BL/6J mice in a dose-dependent manner by inhibiting the MNK-eIF4E signaling pathway, improving lipid metabolism, enhancing mitochondrial function and reducing inflammation, with the 50 mg/kg daily oral dose group showing the most significant effect [1]. HD202A (25-75 mg/kg; orally; single dose) was found to have in vivo inhibitory activity against MNK in mouse white adipose tissue, liver and skeletal muscle 24 hours after administration [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 20 weeks old, average weight approximately 48 g, high-fat diet-induced MASLD) [1]
Doses: 12.5 mg/kg; 25 mg/kg; 50 mg/kg Route of Administration: Oral; once daily; for 11 weeks Experimental Results: Dose-dependently reduced high-fat diet-induced weight gain without affecting food intake. Reduced fat mass and increased lean body mass. Reduced liver and epididymal fat and (at 50 mg/kg only) subcutaneous fat index. Dose-dependently improved glucose homeostasis, with increased glucose clearance and decreased area under the curve (AUC) in the insulin tolerance test (ITT) and oral glucose tolerance test (OGTT) at 50 mg/kg. Within the relevant dose range, fasting blood glucose, serum triglycerides (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), non-esterified fatty acids (NEFA), alanine aminotransferase (ALT), aspartate aminotransferase (AST), and tumor necrosis factor-α (TNF-α) levels were all decreased. Hepatic triglyceride content and fatty macrovesicular degeneration decreased in a dose-dependent manner. At a dose of 50 mg/kg, the hepatic inducible nitric oxide synthase (iNOS) H score decreased, while the hepatic CD163 H score increased (F4/80 level remained unchanged). Hepatic phosphorylated eIF4E (P-eIF4E) levels were inhibited. SCD1 and Plin2 expression were downregulated. ATGL and PGC-1α expression were upregulated. |
| References |
| Molecular Formula |
C25H24N6OS
|
|---|---|
| Molecular Weight |
456.56
|
| CAS # |
2930131-74-9
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(N1CCC(N(C)C)CC1)C2=CC=C(C3=NN4C(S3)=NC=C4C5=CC=C(C#N)C=C5)C=C2
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| HS Tariff Code |
2934.99.9001
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| 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
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|---|---|
| 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 | 2.1903 mL | 10.9515 mL | 21.9029 mL | |
| 5 mM | 0.4381 mL | 2.1903 mL | 4.3806 mL | |
| 10 mM | 0.2190 mL | 1.0951 mL | 2.1903 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.
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