GSK2981278

GSK2981278 is an inverse agonist of retinoic acid receptor-related nuclear receptor gamma (RORgamma, IC50 = 17 nM in a transactivation assay). It is selective for RORgamma over RORalpha. GSK2981278 inhibits IL-17A and IL-22 protein secretion from isolated human peripheral blood T cells grown under Th17 skewing conditions (IC50 = 3.2 nM). Topical application of GSK2981278 (1% ointment) reduces dermal symptoms in a mouse model of psoriasis induced by imiquimod (Cay-14956).Formal Name: N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-benzenesulfonamide. CAS Number: 1474110-21-8. Molecular Formula: C25H35NO5S. Formula Weight: 461.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 5 mg/ml, Ethanol: 15 mg/ml. lambdamax: 246 nm. SMILES: OCC1=CC(S(N(CC(C)C)C2=CC=C(CC)C=C2)(=O)=O)=CC=C1OCC3CCOCC3. InChi Code: InChI=1S/C25H35NO5S/c1-4-20-5-7-23(8-6-20)26(16-19(2)3)32(28,29)24-9-10-25(22(15-24)17-27)31-18-21-11-13-30-14-12-21/h5-10,15,19,21,27H,4,11-14,16-18H2,1-3H3. InChi Key: LZLBRISQTJVZNP-UHFFFAOYSA-N.