864972-30-5

C108297 is a glucocorticoid receptor modulator that prevents both diet-induced obesity and inflammation. C108297 decreased food and fructose intake and increased lipolysis in white adipose tissue (WAT) and free fatty acid levels in plasma, resulting in decreased fat cell size and increased fatty acid oxidation.

C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation[1][2].

[1] Clark RD, et al. 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. Bioorg Med Chem Lett. 2008;18(4):1312-1317. DOI:10.1016/j.bmcl.2008.01.027
[2] van den Heuvel JK, et al. Identification of a selective glucocorticoid receptor modulator that prevents both diet-induced obesity and inflammation. Br J Pharmacol. 2016;173(11):1793-1804. DOI:10.1111/bph.13477