抑制剂描述：

产品名称： GW501516

产品别名：GW-501516,GW 501516,GSK516,GSK 516

信号通路：核受体

靶点：PPARδ

CAS：317318-70-0

靶点活性：

PPARδ,EC50:1.1nM

纯度：>98%

外观：White to off-white solid

保存方法：store at -20℃ for one year（Powder）；
in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.

溶解性：10 mM in DMSO

体外研究：

GW501516, a potent agonist to PPARδ, modulates glyco-metabolism, fatty acid metabolism and alleviates insulin resistance. GW501516 increases fatty acid oxidation by increasing the levels of hepatic mRNAs associated with fatty acid β-oxidation, such as acyl-CoA oxidase (ACOX), carnitine palmitoyltransferase-1 (CPT-1) and liver fatty acid binding protein (L-FABP). In skeletal muscle cells, treatment with GW501516 has been shown to prevent fatty acid-induced inflammation and insulin resistance in by preventing the phosphorylation of insulin receptor substrate-1 at Ser307 and the inhibition of insulin-stimulated Akt phosphorylation, which is caused by exposure to the saturated fatty acid, palmitate. In human liver cells, treatment with GW501516 has been shown to increase the adenosine monophosphate (AMP)/adenosine triphosphate (ATP) ratio and decrease the ATP/adenosine diphosphate (ADP) ratio, thus contributing to the prevention of insulin resistance.

体内研究：Treatment with GW501516 alleviates NAFLD by modulating glucose and fatty acid metabolism.