SR 3335

The retinoic acid receptor-related receptors (RORs) are orphan nuclear receptors with diverse putative roles.{19493,19955,19869} SR 3335 is a selective inverse agonist of ROR?, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM).{21470} It is without effect on ROR?, ROR?, farnesoid X receptor, or liver X receptor ?. SR 3335 evokes ROR?-dependent effects both in vitro and in vivo, altering gene expression as well as gluconeogenesis.{21470}