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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..
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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