1359164-11-6

2-Fluoro-4''-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-[1,1''-biphenyl]-4-methanol was identified as a potent synthetic RORγ-selective modulator.

2-Fluoro-4'-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-[1,1'-biphenyl]-4-methanol was identified as a potent synthetic RORγ-selective modulator.

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 cellsimportant in autoimmune diseases including multiple sclerosisrheumatoid arthritisinflammatory 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 arthritisSR2211 significantly reduced joint inflammationsuppressing inflammatory T cell functionexpression and production of inflammatory cytokinesand macrophage activation.

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