GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORyt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding.{34690} It inhibits the expression of IL-17 (at 0.5 uM) in naïve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORyt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction.
1 mg
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Cayman Chemical
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