| 产品描述： | PGC-1α 抑制剂;PGC-1α Inhibitors;说明：SR-18292可有效抑制PGC-1α葡萄糖异生活性并通过调节GCN5和PGC-1α的相互作用来减少HNF4α的共激活。;InformationSR-18292 SR-18292 inhibits PGC-1α gluconeogenic activity and reduces co-activation of HNF4α by modulating the interaction between GCN5 and PGC-1α.TargetsPGC-1αIn vitroSR-18292 is a potent inhibitor of the gluconeogenic gene expression and glucose production in hepatocytes. It increases the interaction of PGC-1α with GCN5 and reduces co-activation of HNF4α by PGC-1α. SR-18292 suppresses HNF4α/PGC-1α gluconeogenic transcriptional function.In vivoSR-18292 reduces blood glucose, strongly increases hepatic insulin sensitivity and improves glucose homeostasis in dietary and genetic mouse models of type 2 diabetes. SR-18292 suppresses hepatic glucose production and increases liver insulin sensitivity in vivo. The liver is a major target of SR-18292 and probably accounts for a significant part of its anti-diabetic effects.Cell Research(from reference)Cell lines：U-2 OS cells overexpressing Ad-GCN5 Concentrations：10 μM Incubation Time：18 h |
| 靶点： |
PGC-1α |
| 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. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京