1268500-86-2

Upstream product

• 32281-01-9 4-mercapto-2-methylphenol 
• 600-00-0 ethyl 2-bromoisobutyrate 
• 636589-63-4 4-{{2-[4-(trifluoromethyl)phenyl]-4-methylthiazol-5-yl}methylthio}-2-methylphenol 

Downstream Products

• 1026868-55-2 2-methyl-2-{2-methyl-4-[(4-methyl-2-(4-trifluoromethylphenyl)thiazol-5-yl)methylthio]phenoxy}propanoic acid 

Relevant academic research and scientific papers

Synthesis, biological evaluation and molecular modeling of GW 501516 analogues

Eleven analogues of GW 501516 (1) were prepared and subjected to biological testing in a semi-high throughput human skeletal muscle cell assay. The assay testing indicated that all analogues elicited oxidation of oleic acid. Among the most potent agonists, 2e (2-{2-ethyl-4-[(4-methyl-2-(4-trifluoromethylphenyl) thiazol-5-yl)methylthio]phenoxy}-2-methylpropanoic acid), was also subjected to a luciferase-based transfection assay, which showed that this compound is a potent agonist against PPARδ and a moderate agonist against PPARα. Docking of compound 2e into PPARδ revealed that it occupied the agonist binding site and exhibited key hydrogen bonding interactions with His323, His449, and Tyr473. Eleven GW 501516 analogues were prepared and subjected to human skeletal muscle cells. The assay testing indicated that all analogues elicited oxidation of oleic acid. One of the analogues displayed dual agonist effects against both PPARα and PPARδ. Copyright