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GSK805 is a potent, orally bioavailable RORγγ Inhibitor, with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay. GSK805 suppresses T helper 17 (Th17) responses, including IL-17 and IFN-γ production (~ 500 nM). GSK805 directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects. GSK805 induces RORγt binding to Gata3 resulting in increased expression of GATA3. GSK805 reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).
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Animal models | EAE mice |
Formulation | |
Dosages | once daily at 3 doses (1, 3, and 10 mg/kg) |
Administration | orally |
Molecular Weight | 532.36 |
Formula | C23H18Cl2F3NO4S |
CAS Number | 1426802-50-7 |
Solubility (25°C) | DMSO 100 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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