SR3335

The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles. SR 3335 is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (K_i = 220 nM) and inhibiting constitutive transactivation activity (IC₅₀ = 480 nM). It is without effect on RORβ, RORγ, farnesoid X receptor, or liver X receptor α. SR 3335 evokes RORα-dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis.