| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
STA-013 (5 µM) inhibited the activities of EphB1 (54%), EphB2 (42%), EphB4 (52%), SGK1 (47%) and PKBb (43%) by kinase profiling analysis, while having no effect on the remaining 140 kinases [1]. STA-013 (0.032–20 µM, 96 h) significantly inhibited lipid accumulation in embryonic mouse 3T3-L1 cells in a dose-dependent manner [1]. STA-013 (1 µM, 30 min) significantly reduced basal respiration, proton leakage, ATP production and nonmitochondrial oxygen consumption in 3T3-L1 cells, increased maximal respiration and reserve respiration capacity, significantly enhanced glycolysis and glycolytic capacity, and reduced palmitic acid oxidation level [1].
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| ln Vivo |
STA-013 (12.5, 25, and 50 mg/kg, intraperitoneal injection, once daily for 6 weeks) promoted weight loss, diabetes clearance, and insulin iconography in a high-fat diet-induced C57BL/6J electrode, and improved insulin signaling in isolated brown adipose tissue and abdomen [1]. The weight loss sensed by STA-013 (12.5, 25, and 50 mg/kg, intraperitoneal injection, once daily for 6 weeks) in a DIO electrode was not achieved by reducing food intake or increasing intake rate [1].
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| Animal Protocol |
Animal/Disease Models: HFD (for 10 weeks) induced male C57BL/6J mice (16-20 weeks old)[1]
Doses: 12.5, 25 and 50 mg/kg Route of Administration: i.p., daily for 6 weeks Experimental Results: Showed a significant reduction in whole-body weight, improved glucose clearance in the IP glucose tolerance test (GTT), and insulin sensitivity in the IP insulin tolerance test (ITT). Showed a significant reduction in the fat mass associated with preserving the lean muscle mass in HFD-obese mice. Induced intrascapular brown adipose tissue (BAT)-specific thermogenesis in HFD obese mice. Showed significant reduction in whole-body weight associated with reduction in the fat mass (%) as well as increase in the lean mass (%), improved glucose clearance, and restored insulin sensitivity in HFD obese mice. Inhibited phosphorylation of ephb tyrosine kinase forward signaling in both the liver and BAT at 25 mg/kg. Increased the p-AKT/AKT signaling, which suggests the activation of insulin signaling in BAT and liver in HFD obese mice. Increased insr-β protein levels compared to vehicle in BAT and liver lysates. Animal/Disease Models: HFD (for 10 weeks) induced male C57BL/6J DIO mice (16-20 weeks old)[1] Doses: 12.5, 25 and 50 mg/kg Route of Administration: i.p., daily for 6 weeks Experimental Results: Significantly increased oxygen (VO 2 and carbon dioxide (VCO 2) consumption ) production in the light cycle. Decreased profile in the respiratory exchange rates (RER) during the dark cycle. Decrease in the total energy expenditure (EE) for STA- 013 treated HFD mice. Induced weight loss occurred without a change in food intake, suggesting it was due to an elevated metabolic rate. |
| References |
| Molecular Formula |
C24H17N3O2S
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|---|---|
| Molecular Weight |
411.48
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| Appearance |
Typically exists as solids at room temperature
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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)
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| 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 | 2.4303 mL | 12.1513 mL | 24.3025 mL | |
| 5 mM | 0.4861 mL | 2.4303 mL | 4.8605 mL | |
| 10 mM | 0.2430 mL | 1.2151 mL | 2.4303 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.