GSK805 (C09-1135-915)

GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC 50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunityIn VitroGSK805 (0.5 μM; 4 d) inhibits Th17 cell responses. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Differentiation AssayCell Line: CD4 + T cells Concentration: 0.5 μM Incubation Time: 4 days Result: Inhibited IL-17 production during Th17 cell differentiation.In VivoGSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE). GSK805 (30 mg/kg; p.o. once) inhibits Th17 cell responses in EAE mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 mice were immunized with MOG35–55 plus CFADosage: 10 mg/kg Administration: Oral gavage; 10 mg/kg once per day; for 35 days Result: Efficiently ameliorated the severity of EAE in mice. Animal Model: C57BL/6 mice with EAEDosage: 30 mg/kg Administration: Oral gavage; 30 mg/kg once Result: Reduced both IFN-γ - IL-17 + and IFN-γ + IL-17 + T cells without altered the frequency of TNF-α + T cells in EAE mice.IC50& Target:IC50: 8.4 (RORγt). Specification: 10mM in DMSO Molecular Formula: C23H18Cl2F3NO4S Molecular Weight: 532.4