Selective RORα partial inverse agonist (IC50 = 480 nM) – displays no activity at RORß, RORγ, or FXR. It was able to suppress gluconeogenesis in diet-induced obese mice. SR3335 was able to upregulate uncoupling protein 1 (UCP1), a unique mitochondrial protein devoted to thermogenesis, in wild...
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Selective RORα partial inverse agonist (IC50 = 480 nM) – displays no activity at RORß, RORγ, or FXR. It was able to suppress gluconeogenesis in diet-induced obese mice. SR3335 was able to upregulate uncoupling protein 1 (UCP1), a unique mitochondrial protein devoted to thermogenesis, in wild type mice leading to decreased body weight and fat mass. It inhibited the development of mouse and human TH17 cells in vitro and in vivo leaving thymic T cells intact. SR3335’s ability to block pathogenic, but not protective TH17 cell function makes it an important new tool in the study of TH17-mediated inflammatory and autoimmune diseases
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