SR 1001

Retinoic-acid-receptor-related orphan receptors (ROR) alpha and gamma play a key role in the development of T-helper cells that produce interleukin-17 (TH17 cells), a subset of CD4+ T-cells that contribute to the inflammatory process and have been implicated in the pathology of autoimmune diseases. SR 1001 is a synthetic ligand specific for RORalpha and RORgamma (Kis = 172 and 111 nM, respectively) that functions as an inverse agonist at these receptors. SR 1001 has been shown to suppress IL-17 promoter driven transcriptional activity by inhibiting the interaction of co-activators such as TRAP220 nuclear receptor box 2 peptide (IC50 = 117 nM) and SRC2 with RORalpha and RORgamma as well as by increasing the recruitment of corepressors such as NCoR. At 5 µM, SR 1001 inhibits TH17 cell differentiation and IL-17A secretion in cultured splenocytes and human PBMCs. A 25 mg/kg dose of SR 1001 twice/day delays the onset and the severity of experimental autoimmune encephalomyelitis, a mouse model of multiple sclerosis.Formal Name: N-(5-(N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)sulfamoyl)-4-methylthiazol-2-yl)acetamide. CAS Number: 1335106-03-0. Molecular Formula: C15H13F6N3O4S2. Formula Weight: 477.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:10): 0.1 mg/ml. lambdamax: 235, 282 nm. SMILES: CC(NC1=NC(C)=C(S(NC2=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C2)(=O)=O)S1)=O. InChi Code: InChI=1S/C15H13F6N3O4S2/c1-7-11(29-12(22-7)23-8(2)25)30(27,28)24-10-5-3-9(4-6-10)13(26,14(16,17)18)15(19,20)21/h3-6,24,26H,1-2H3,(H,22,23,25). InChi Key: OZBSSKGBKHOLGA-UHFFFAOYSA-N. License: Sold under license from The Scripps Research Institute..