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SR 2211 is a potent and selective inverse agonist of RORγ with IC50 value of 320 nM [1].

RAR-related orphan receptor gamma (RORγ) is a nuclear receptor and a DNA-binding transcription factor. RORγ plays an important role in the regulation of circadian rhythms and Th17 cell differentiation [2].

SR 2211 is a potent and selective RORγ inverse agonist. SR2211 bound to RORγ with Ki value of 105 nM. SR2211 (10 μM) inhibited RORγ activity by 90% but didn’t affect the transcriptional activity of RORα and farnesoid X receptors (FXR). SR2211 showed weak activation of liver X receptor α (LXRα). In EL-4 murine T lymphocyte cell line, SR2211 (5 μM) followed by PMA/ionomycin significantly inhibited the expression of IL-17 and IL-23 receptor in a dose-dependent way [1]. Enriched naive CD4+ T cells under Th17 polarizing conditions, SR2211 significantly inhibited the production of IL-17, which suggested that SR2211 inhibited Th17 cell differentiation. In LPS-stimulated RAW 264.7 cells, SR2211 (5 μM) inhibited the expression of TNFα, IL-1β and IL-6, the proinflammatory cytokines that played an important role in the pathogenesis of RA [2].

Of the CIA mouse model, SR2211 (20 mg/kg) inhibited the development of arthritis in a dose-dependent way [2].

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