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Drug intelligence / Profile preview
GSK3787
- Development stage
- Preclinical
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
GSK3787 is a selective, high-affinity, and irreversible antagonist of peroxisome proliferator-activated receptor delta (PPARδ, also known as PPARβ). Developed by GSK, it acts by covalently modifying the receptor at the Cys249 residue, thereby blocking agonist-induced transcriptional activity without affecting basal activity in most cell types. GSK3787 displays no measurable affinity for PPARα or PPARγ. It is widely utilized as a chemical probe in preclinical research to investigate the physiological and pathological roles of PPARδ in lipid metabolism, glucose homeostasis, inflammation, and various cancers.
- Other names
- 4-chloro-N-[2-[5-(trifluoromethyl)pyridin-2-yl]sulfonylethyl]benzamide4-chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamidePT-S58PT-S-58PT-S 58
02
Targets
ANGPTL4 (Angiopoietin-like 4)PPARG (Peroxisome proliferator-activated receptor gamma)PPARD (Peroxisome proliferator–activated receptor delta)
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