Drug intelligence / Profile preview

GW7647

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Intracerebroventricular, Intracerebral
01

Overview

GW7647 is a potent and highly selective small molecule agonist of the peroxisome proliferator-activated receptor alpha (PPARα). Developed by GSK, it exhibits an EC50 of 6 nM for PPARα, demonstrating over 100-fold selectivity over the PPARγ and PPARδ isoforms. As a research tool, it is widely used to investigate the role of PPARα in lipid metabolism, inflammation, and metabolic disorders. GW7647 has shown lipid-lowering activity in animal models of dyslipidemia and has been studied for potential neuroprotective effects in Alzheimer's disease due to its ability to cross the blood-brain barrier. In oncology research, it has been shown to sensitize hepatocellular carcinoma cells to genotoxic drugs by modulating the p53 acetylation/phosphorylation status through the activation of the PPARα/p300 signaling axis. It is not approved for human clinical use.

Other names
2-[[4-[2-[[[(cyclohexylamino)carbonyl](4-cyclohexylbutyl)amino]ethyl]phenyl]thio]-2-methylpropanoic acidCAS 265129-71-3CAS265129-71-3CAS-265129-71-3
02

Targets

PPARD (Peroxisome proliferator–activated receptor delta)PPARA (Peroxisome proliferator-activated receptor alpha)PPARG (Peroxisome proliferator-activated receptor gamma)

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