SR1001

SR1001 is a selective ROR_α and ROR_γt inverse agonist with K_is 172 and 111 nM, respectively. In Vitro: SR1001 inhibits the development of murine T_H17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with ROR_γ in a dose dependent manner (IC₅₀ value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human T_H17 cells^[1]. In Vivo: SR1001 effectively suppresses the clinical severity of autoimmune disease in mice. Administration of SR1001 to C57BL/6 mice suppresses the expression of hepatic ROR target genes, Cyp7b1, Rev-erbα, and Serpine 1^[1]. SR1001 a ROR_α inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice^[2].