S88275 |
MSDC-0602 |
| 源叶(MedMol) | 97% |
- 产品描述： Azemiglitazone (MSDC-0602) 是一种直接的线粒体丙酮酸载体 (mitochondrial pyruvate carrier, MPC) 抑制剂，可调节小鼠和人类的中央碳代谢
- 靶点： MPC
- 体外研究： Azemiglitazone (MSDC-0602) is a modified hiazolidinediones (TZDP) with alterations in the carbon backbone that limit the ability to bind PPARγ, with the IC50 for PPARγ of 18.25 μM. Azemiglitazone (MSDC-0602) also shows the affinity for mitochondrial binding, with the IC50 of 1.38 μM. Using a Gal4-PPARγ construct containing the ligand binding domain of mouse PPARγ, MSDC-0602 only minimally activates Gal4-PPARγ in HepG2 cells even at a concentration of 50 μM.
- 体内研究： Azemiglitazone (MSDC-0602) corrects plasma glucose, nonesterified fatty acids, triglycerides, cholesterol, and insulin concentrations, which are elevated in ob/ob mice compared with lean controls. Treatment with Azemiglitazone (MSDC-0602) also significantly improved glucose and insulin tolerance in ob/ob mice
- 细胞实验： Cell lines: HepG2 hepatoma cells Concentrations: 0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM and 50μM Incubation Time: 48 h Method: HepG2 hepatoma cells were co-transfected by calcium phosphate coprecipitation with expression vectors for Gal4-PPARγ (ligand binding domain only) or Gal4-PPARα, heterologous firefly luciferase reporter construct driven by five copies of a Gal4 response element, and SV40-driven renilla luciferase reporter construct. Transfected cells were treated with PPARγ agonists (rosiglitazone and pioglitazone), PPARα agonist (GW7647), or MSDC-0602 for 24 h. Cell lysate firefly and renilla luciferase activity was assessed 48 h later by using the Dual-Glo kit. Firefly luciferase activity was corrected for renilla luciferase activity, and DMSO (vehicle) values were normalized to 1.0.
- 参考文献：
1. ADAM J. RAUCKHORST, et al. Diabetes 2021 Jun; 70(Supplement 1) 2. Chen Z, et al. Insulin resistance and metabolic derangements in obese mice are ameliorated by a novel peroxisome proliferator-activated receptor γ-sparing thiazolidinedione. J Biol Chem. 2012 Jul 6;287(28):23537-48.
- 溶解性： DMSO : 125 mg/mL (336.56 mM; Need ultrasonic)；H2O : < 0.1 mg/mL (insoluble)
- 保存条件： -20°C
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.692 ml 13.462 ml 26.925 ml 5 mM 0.538 ml 2.692 ml 5.385 ml 10 mM 0.269 ml 1.346 ml 2.692 ml 50 mM 0.054 ml 0.269 ml 0.538 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
