| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
SKLB-11A enhances the deacetylation activity of SIRT3, with an EC50 value of 21.95 μM[1]. SKLB-11A (0.625–5 μM; 24 h) does not alter SIRT3 protein levels but significantly enhances SIRT3 activity in H9c2 cells[1]. SKLB-11A has a high affinity for SIRT3 and enhances its interaction with p53-Ac substrates[1]. SKLB-11A (5–20 μM; 24 h) alleviates doxorubicin-induced mitochondrial damage in H9c2 cells and promotes SIRT3-mediated autophagy[1].
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| ln Vivo |
Pretreatment with SKLB-11A (10–20 mg/kg; by gavage; daily; for 7 days) inhibited doxorubicin-induced cardiac dysfunction in mice[1]. Treatment with SKLB-11A (20 mg/kg; by gavage; daily; for 7 days) reduced ischemia/reperfusion (I/R)-induced myocardial injury in mice[1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: H9c2 cells Tested Concentrations: 0.625 μM, 1.25 μM, 2.5 μM, 5 μM Incubation Duration: 24 hours Experimental Results: Induced deacetylation at K122 and K68 sites, thereby enhancing MnSOD enzyme activity. Activated deacetylation of endogenous SIRT3 in H9c2 cells. Western Blot Analysis [1] Cell Types: H9c2 cells Tested Concentrations: 5 μM, 10 μM, 20 μM Incubation Duration: 24 hours Experimental Results: Increased LC3-II expression and decreased p62 level indicated enhanced autophagy flux. Increased expression of PINK1 and Parkin promoted co-localization of mitochondria with Parkin and LC3-II. |
| Animal Protocol |
Animal/Disease Models:Male C57BL/6J mice (8 weeks old, approximately 23 g) [1]
Doses: 10 and 20 mg/kg/day Route of Administration: Gavage; once daily for 7 days; followed by intraperitoneal injection of doxorubicin for 2 weeks Experimental Results: Significantly restored left ventricular ejection fraction (EF) and fractional shortening (FS) in a dose-dependent manner. Partially reversed doxorubicin-induced weight loss and reduced serum markers of myocardial injury, including LDH, CK-MB, and BNP. Protected myocardial structure and reduced pathological damage. No significant toxicity was observed at effective doses, as confirmed by histological examination of the heart, liver, spleen, lungs, and kidneys. Animal/Disease Models:Male C57BL/6J mice (8-12 weeks old) were induced with myocardial ischemia-reperfusion (I/R) injury [1]. Doses: 20 mg/kg Route of Administration: Gavage; once daily for 7 days Experimental Results: The mice recovered cardiac dysfunction induced by I/R injury. They partially reversed the elevation of serum myocardial injury markers (including LDH, CK-MB, and BNP) induced by I/R. They significantly reduced I/R-induced myocardial fibrosis. |
| References |
| Molecular Formula |
C19H15FN4O2
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|---|---|
| Molecular Weight |
350.35
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| CAS # |
433953-86-7
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| Appearance |
Light yellow to yellow solid
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| SMILES |
COC(C1=C(N)N(CC2=CC=C(F)C=C2)C3=NC4=CC=CC=C4N=C31)=O
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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) |
DMSO : ~7.78 mg/mL (~22.21 mM; with sonication)
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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 | 2.8543 mL | 14.2714 mL | 28.5429 mL | |
| 5 mM | 0.5709 mL | 2.8543 mL | 5.7086 mL | |
| 10 mM | 0.2854 mL | 1.4271 mL | 2.8543 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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