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Product Name | SR 1001 |
Description | Purity >98%. 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 (TH 17 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 (Ki s = 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 TH 17 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. |
Size | n/a |
Concentration | n/a |
Applications | n/a |
Other Names | N-(5-(N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)sulfamoyl)-4-methylthiazol-2-yl)acetamide |
Gene, Accession, CAS # | CAS: 1335106-03-0 |
Catalog # | LS-H10006 |
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Order / More Info | SR 1001 from LIFESPAN BIOSCIENCES INC. |
Product Specific References | n/a |
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