GSK805

GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORgammat) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding. It inhibits the expression of IL-17 (at 0.5 µM) in naïve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORgammat-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.Formal Name: N-[2,6-dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)-benzeneacetamide. CAS Number: 1426802-50-7. Molecular Formula: C23H18Cl2F3NO4S. Formula Weight: 532.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 221, 256 nm. SMILES: ClC1=CC(NC(CC2=CC=C(S(CC)(=O)=O)C=C2)=O)=CC(Cl)=C1C3=C(OC(F)(F)F)C=CC=C3. InChi Code: InChI=1S/C23H18Cl2F3NO4S/c1-2-34(31,32)16-9-7-14(8-10-16)11-21(30)29-15-12-18(24)22(19(25)13-15)17-5-3-4-6-20(17)33-23(26,27)28/h3-10,12-13H,2,11H2,1H3,(H,29,30). InChi Key: CEICQMBWAQAIQX-UHFFFAOYSA-N.