| Bioactivity | SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively. | ||||||||||||
| Invitro | 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[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 RORα inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice[2]. | ||||||||||||
| Name | SR1001 | ||||||||||||
| CAS | 1335106-03-0 | ||||||||||||
| Formula | C15H13F6N3O4S2 | ||||||||||||
| Molar Mass | 477.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Solt LA, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4. [2]. Crumbley C, et al. Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα). PLoS One. 2012;7(4):e33804. |