GSK-4716 是一种ERRβ/γ选择性激动剂。

GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand

GSK4716 was a selective ERRbeta/gamma agonist[1].?ERRbeta is transiently induced, and ERRgamma is dramatically induced (and accumulates) in a differentiation-dependent manner in skeletal muscle cells.?Treatment of differentiated skeletal muscle cells with the ERRbeta/gamma agonist (GSK4716) produced a significant increase in the expression of GRalpha (isoform D) .the mRNAs encoding the glucocorticoid receptor (GR), 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1), the enzyme that converts inactive cortisone to cortisol and hexose-6-phosphate dehydrogenase expression (H6PDH) that stimulates oxoreduction by 11beta-HSD1.the mRNAs encoding characterized GR target genes, including C/EBP, ApoD and Monoamine oxidase-A (MAO-A) are induced in GSK4716 treated cells[2].GSK4716 has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise[3]

Mouse myoblasts were isolated as described previously.?Human ERRγ-IRES green fluorescent protein adenovirus was generated by Welgen.?Following a 48-h differentiation period, myotubes were transduced with green fluorescent protein or ERRγ adenovirus for 48 h. The titers to achieve low and high levels of ERRγ expression were 1* 10^8 and 5*10^8 virus particles/ml, respectively.?GSK4716 was synthesized as described previously and dissolved in DMSO for cell culture experiments.?Cells treated with a corresponding volume of DMSO were used as controls[3]

101574-65-6

C17H18N2O2

282.34

DMSO:100 mg/mL (354.18 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years