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| Product | Description | |
|---|---|---|
| SR1001 | Retinoic-acid-receptor-related orphan receptors (ROR) α and γ 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 RORα and RORγ (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 RORα and RORγ 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. Group: Pharmaceutical. Alternative Names: SR 1001; SR-1001. CAS No. 1335106-03-0. Pack Sizes: 100 mg. Product ID: B1370-463179. Molecular formula: C15H13F6N3O4S2. Mole weight: 477.4. Custom synthesis is available. Send your inquiries for more information. |  London |
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