Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 38.00 | |
10 mg | In stock | $ 58.00 | |
25 mg | In stock | $ 131.00 | |
50 mg | In stock | $ 252.00 | |
100 mg | In stock | $ 469.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 41.00 |
Description | GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand |
In vitro | 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] |
Cell Research | 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] |
Molecular Weight | 282.34 |
Formula | C17H18N2O2 |
CAS No. | 101574-65-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (354.18 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GSK-4716 101574-65-6 Endocrinology/Hormones Estrogen Receptor/ERR GSK4716 inhibit GSK 4716 Inhibitor inhibitor