1207192-76-4Relevant academic research and scientific papers
Identification and characterization of 4-chloro-N-(2- {[5-trifluoromethyl)- 2-pyridyl] sulfonyl} ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist
Shearer, Barry G.,Wiethe, Robert W.,Ashe, Adam,Billin, Andrew N.,Way, James M.,Stanley, Thomas B.,Wagner, Craig D.,Xu, Robert X.,Leesnitzer, Lisa M.,Merrihew, Raymond V.,Shearer, Todd W.,Jeune, Michael R.,Ulrich, John C.,Wilison, Timothy M.
, p. 1857 - 1861 (2010)
4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide 3 (GSK3787) was identified, as a potent and selective ligand for PPARδ with good pharmacokinetic properties. A detailed binding study using mass spectral, analysis confirmed covalent binding to Cys249 within the PPARδ binding pocket. Gene expression studies showed that pyridylsulfone 3 antagonized the transcriptional activity of PPARδ and inhibited basal CPT1 a gene transcription. Compound 3 is a PPARδ antagonist with utility as a tool to elucidate PPARδ cell biology and pharmacology.
