SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.
体外研究
SR1001 inhibits the development of murine TH17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner (IC50 value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human TH17 cells.
体内研究
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. SR1001 a RORα inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice.
分子式
C15H13F6N3O4S2
分子量
477.40
CAS号
1335106-03-0
运输条件
Room temperature in continental US; may vary elsewhere.