S88567 |
SR-18292 |
| 源叶(MedMol) | 98% |
- 产品描述：
SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
- 靶点： PGC-1α
- 体外研究：
The transcriptional coactivator PGC-1α plays a pivotal role in energy homeostasis by co-activating transcription factors that regulate fat and glucose metabolism. SR-18292 increases the interaction of PGC-1α with the acetyl transferase GCN5 and reduces co-activation of nuclear hormone receptor HNF4α by PGC-1α. SR-18292 suppresses HNF4α/PGC-1α gluconeogenic transcriptional function. By increasing the interaction of GCN5 with PGC-1α, SR-18292 increases the acetylation of specific PGC-1α lysine residues that might subsequently decrease its gluconeogenic activity.
- 体内研究：
SR-18292 reduces fasting blood glucose, increases hepatic insulin sensitivity and improves glucose homeostasis in diabetic mice. The high fat diet (HFD) fed mice, a dietary model of obesity and T2D, are treated with SR-18292 (45mg/kg) via I.P. injection for 3 consecutive days and again on day 4 before measuring fasting blood glucose. Strikingly, mice that are treated with SR-18292 have significantly lower levels of fasting blood glucose concentrations compared to matched vehicle-treated control mice. The induction of gluconeogenic gene expression is a regulatory component of the response to fasting. Importantly, gluconeogenic gene expression, specifically that of Pck1, is inhibited in livers isolated from mice treated with SR-18292.
- 参考文献：
1. Sharabi K, et al. Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017 Mar 23;169(1):148-160.e15.
- 溶解性： Soluble in DMSO、Ethanol
- 保存条件： -20°C
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.729 ml 13.643 ml 27.285 ml 5 mM 0.546 ml 2.729 ml 5.457 ml 10 mM 0.273 ml 1.364 ml 2.729 ml 50 mM 0.055 ml 0.273 ml 0.546 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
