Biochem/physiol Actions

SR2211 (ML310) is a potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (RORγ). RORγ is essential for interleukin 17 expression and differentiation of TH17 cells, important in autoimmune diseases including multiple sclerosis, rheumatoid arthritis, inflammatory bowel disease and lupus. SR2211 (ML310) treatment of EL-4 murine T lymphocyte cells resulted in suppression of gene expression and production of IL-17 with an IC₅₀ ~320 nM with no effect on the transcriptional activity of RORγ. In a mouse model of rheumatoid arthritis, SR2211 significantly reduced joint inflammation, suppressing inflammatory T cell function, expression and production of inflammatory cytokines, and macrophage activation.

Packaging

5, 25 mg in glass bottle