SKLB-11A
Based on 1 Customer Validation
SKLB-11A is a selective, orally active and allosteric SIRT3 (sirtuin 3) agonist with a Kd value of 4.7 μM. SKLB-11A is highly selective for other members of the SIRT family. SKLB-11A activates autophagy-related signaling pathways, prevents mitochondrial dysfunction, improves cardiac function in Doxorubicin (HY-15142A)-induced cardiotoxicity and myocardial ischemia/reperfusion models.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.40%
- CAS 番号: 433953-86-7
- 分子式: C19H15FN4O2
- 分子量:350.35
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
|
SIRT3 4.7 μM (Kd) |
SKLB-11A enhances SIRT3 deacetylation activity with an EC50 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 binds to SIRT3 with high affinity and enhances its interaction with the p53-Ac substrate[1].
SKLB-11A (5-20 μM; 24 h) ameliorates Doxorubicin-induced mitochondrial damage and promotes SIRT3-mediated autophagy in H9c2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:H9c2 cells
-
Concentration:0.625 μM, 1.25 μM, 2.5 μM, 5 μM
-
Incubation Time:24 h
-
Result:Induced deacetylation at K122 and K68, resulting in enhanced MnSOD enzymatic activity.
Activated endogenous SIRT3 deacetylation in H9c2 cells.
-
Cell Line:H9c2 cells
-
Concentration:5 μM, 10 μM, 20 μM
-
Incubation Time:24 h
-
Result:Increased LC3-II expression and reduced p62 levels, indicating enhanced autophagic flux.
Increased the expression of PINK1 and Parkin, and promoted colocalization of mitochondria with Parkin and LC3-II.
SKLB-11A (20 mg/kg; oral gavage; daily; for 7 days) treatment alleviated ischemia/reperfusion (I/R)-induced myocardial injury in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male C57BL/6J mice (8 weeks, ~23 g)[1]
-
Dosage:10 and 20 mg/kg/day
-
Administration:Oral gavage; daily; for 7 days; then injected Doxorubicin intraperitoneally for 2 weeks
-
Result: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.
Preserved myocardial structure and alleviated pathological damage.
Demonstrated no apparent toxicity at effective doses, as evidenced by preserved organ histology in the heart, liver, spleen, lungs, and kidneys.
-
Animal Model:Male C57BL/6J mice (8-12 weeks old) was induced myocardial ischemia-reperfusion (I/R) injury[1].
-
Dosage:20 mg/kg
-
Administration:Oral gavage; daily; for 7 days
-
Result:Restored cardiac function impaired by I/R injury.
Partially reversed I/R-induced elevations in serum myocardial injury markers, including LDH, CK-MB, and BNP.
Markedly reduced I/R-induced cardiac fibrosis.
化学情報
-
CAS 番号 433953-86-7
-
性状 Solid
-
分子量 350.35
-
分子式 C19H15FN4O2
-
Color Light yellow to yellow
-
SMILES
COC(C1=C(N)N(CC2=CC=C(F)C=C2)C3=NC4=CC=CC=C4N=C31)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 7.78 mg/mL (22.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (280 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8543 mL | 14.2714 mL | 28.5429 mL | 71.3572 mL |
| 5 mM | 0.5709 mL | 2.8543 mL | 5.7086 mL | 14.2714 mL | |
| 10 mM | 0.2854 mL | 1.4271 mL | 2.8543 mL | 7.1357 mL | |
| 15 mM | 0.1903 mL | 0.9514 mL | 1.9029 mL | 4.7571 mL | |
| 20 mM | 0.1427 mL | 0.7136 mL | 1.4271 mL | 3.5679 mL |