1207192-78-6Relevant articles and documents
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.
experimental part, p. 1857 - 1861 (2010/08/22)
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.
