GSK5182 Chemical Properties

Boiling point:

567.6±50.0 °C(Predicted)

Density 

1.132±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO:54.5(Max Conc. mg/mL);130.52(Max Conc. mM)
Ethanol:84.0(Max Conc. mg/mL);201.17(Max Conc. mM)

pka

10.27±0.15(Predicted)

form 

Solid

color 

Off-white to light yellow

GSK5182 Usage And Synthesis

Biological Activity

GSK5182 is an orally available 4-hydroxy-tamoxifen (4-OHT) analog and a high affinity estrogen receptor-related receptor γ (ERRγ) inverse agonist (68% inhibition at 1 μM by reporter assay) with 25-fold reduced affinity and little antagonistic activity toward ERRα (No inhibition against 100 nM estradiol-induced reporter activity up to 1 μM). GSK5182 effectively inhibits ERRγ-dependent gene expression and biological functions both in cultures (1-10 μM) and in various animal studies in vivo (10-80 mg/kg i.p. or p.o. in rats and mice).