SR1555 hydrochloride is a selective RORγ inverse agonist (IC50=1.5 uM) that suppresses T(H)17 cells and stimulates T regulatory cells.
SR1555 is devoid of LXR, FXR, and RORα activity, displaces [3H]T0901317 from the ligand binding domain (LBD) of RORγ with IC50 of 1 uM.
SR1555 represses the expression of RORγ while leading to increased expression of FGF21 and adipoQ in pre-adipocyctes.
SR1555 inhibits activation of hormone-sensitive lipase and increased fatty acid oxidation in obese diabetic mice.
