SR-18292

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SR-18292 是一种 PPAR gamma coactivator-1α (PGC-1α) 抑制剂，可增加 PGC-1α 乙酰化，抑制糖异生基因表达并减少肝细胞中葡萄糖的产生。

SR-18292 is a PGC-1α inhibitor. SR-18292 reduces blood glucose, strongly increases hepatic insulin sensitivity, and improves glucose homeostasis in dietary and genetic mouse models of T2D.

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.

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.

SR-18292 | SR 18292 | SR18292

Cell Cycle/DNA Damage

HDAC

PGC-1α

Metabolic Disease

——

2095432-55-4

366.51

C23H30N2O2

>98% (HPLC)

DMSO : ≥ 100 mg/mL; 272.85 mM

CC(C)(C)N(Cc1ccc(C)cc1)CC(O)COc3cccc2nccc23

1-((1H-indol-4-yl)oxy)-3-(tert-butyl(4-methylbenzyl)amino)propan-2-ol

(-20℃)

With Ice Pack

≥ 2 years