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 (Ki = 220 nM) and inhibiting constitutive transactivation activity (IC50 = 480 nM). It has no 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.
Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Endocrinology and Metabolic Disease | ROR
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