PPARbeta/delta Antagonist, GSK3787 – CAS 188591-46-0 – Calbiochem

Descrição detalhada : A cell-permeable pyridylsulfone that acts as a selective, high affinity PPARbeta (PPARdelta) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARbeta and >10 µM against PPARalpha or PPARgamma) and effectively antagonizes agonist-induced, but not basal, PPARbeta transcription activity both in cultures in vitro (IC50 = 126 nM in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium; 10 mg/kg GSK3787; p.o.) by covalently modifying PPARbeta at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARgamma (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively)., A cell-permeable and orally available pyridylsulfone compound that acts as a selective, high affinity PPARbeta (PPARdelta) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARbeta and >10 µM against PPARalpha or PPARgamma) and effectively antagonizes agonist-induced, but not basal, PPARbeta transcription activity both in cultures in vitro (IC50 = 126 nM against 2 nM GW501516-induced reporter transcription in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium by 10 mg/kg GSK3787; p.o.) by covalently modifying PPARbeta at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARgamma (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).
Sinónimos : PPARbeta/delta Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem; 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl)sulfonyl)ethyl)benzamide, PPARbeta Antagonist I, PPARdelta Antagonist I
Fórmula molecula r: C15H12ClF3N2O3S
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X10MG