PPARβ/δ antagonist,novel and irreversible
CAS：188591-46-0
分子式：C15H12ClF3N2O3S
分子量：392.78
纯度：98%
存储：Store at -20°C

Background:

GSK3787 is a novel and irreversible antagonist of the peroxisome proliferator-activated receptor-β/δ (PPAR-β/δ) that covalently binds to a cysteine residue in the ligand-binding domain of PPAR- β/δ. Although it responses to ligand activation to modulate the association of both PPAR-β/δ and PPAR-γ coregulator peptides, GSK3787 exhibits considerably higher antagonism of PPAR-β/δ than that of PPAR-γ. Results of recent studies have shown that oral administration of GSK3787 results in the antagonism of GW0742-induced overexpression of Angptl4 and Adrp mRNA in wild-type mouse colon, which is correlated with reduced promoter occupancy of PPAR-β/δ on the Angptl4 and Adrp genes.

Reference

[1].Palkar PS, Borland MG, Naruhn S, Ferry CH, Lee C, Sk UH, Sharma AK, Amin S, Murray IA, Anderson CR, Perdew GH, Gonzalez FJ, Müller R, Peters JM. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. Mol Pharmacol. 2010;78(3):419-430