The retinoic acid receptor-
related receptors (RORs) are orphan nuclear receptors with diverse putative roles.
1,2,3 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 (IC
50 = 480 nM).
4 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.
4 
