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Description

A cell-permeable, orally available, non-toxic, conformationally restricted biaryl-amide compound that acts as a potent retinoid-related orphan receptor gammat (RORgammat) isoform selective inverse agonist and suppresses T helper 17 (Th17) responses, including IL-17 and IFN-gamma production (~ 500 nM). Directly and reversibly interacts with the ligand binding domain of RORgammat to block its transcriptional effects, however, it does not affect RORgammat binding to DNA. Induces RORgammat binding to Gata3 resulting in increased expression of GATA3. Reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).Please note that the molecular weight for this compound is batch-specific due to variable water content., A cell-permeable, orally available, non-toxic, conformationally restricted biaryl-amide compound that acts as a potent retinoid-related orphan receptor gammat (RORgammat) isoform selective inverse agonist and suppresses T helper 17 (Th17) responses, including IL-17 and IFN-gamma production (~ 500 nM). Directly and reversibly interacts with the ligand binding domain of RORgammat to block its transcriptional effects, however, it does not affect RORgammat binding to DNA. Induces RORgammat binding to Gata3 resulting in increased expression of GATA3. Reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).