| CAS NO: | 1359164-11-6 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1359164-11-6 |
| 化学名 | 1,1,1,3,3,3-hexafluoro-2-(2-fluoro-4'-((4-(pyridin-4-ylmethyl)piperazin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)propan-2-ol |
| Canonical SMILES | FC1=CC(C(C(F)(F)F)(C(F)(F)F)O)=CC=C1C2=CC=C(C=C2)CN3CCN(CC4=CC=NC=C4)CC3 |
| 分子式 | C26H24F7N3O |
| 分子量 | 527.48 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SR 2211 is a potent and selective inverse agonist of RORγ with IC50 value of 320 nM [1]. RAR-related orphan receptor gamma (RORγ) is a nuclear receptor and a DNA-binding transcription factor. RORγ plays an important role in the regulation of circadian rhythms and Th17 cell differentiation [2]. SR 2211 is a potent and selective RORγ inverse agonist. SR2211 bound to RORγ with Ki value of 105 nM. SR2211 (10 μM) inhibited RORγ activity by 90% but didn’t affect the transcriptional activity of RORα and farnesoid X receptors (FXR). SR2211 showed weak activation of liver X receptor α (LXRα). In EL-4 murine T lymphocyte cell line, SR2211 (5 μM) followed by PMA/ionomycin significantly inhibited the expression of IL-17 and IL-23 receptor in a dose-dependent way [1]. Enriched naive CD4+ T cells under Th17 polarizing conditions, SR2211 significantly inhibited the production of IL-17, which suggested that SR2211 inhibited Th17 cell differentiation. In LPS-stimulated RAW 264.7 cells, SR2211 (5 μM) inhibited the expression of TNFα, IL-1β and IL-6, the proinflammatory cytokines that played an important role in the pathogenesis of RA [2]. Of the CIA mouse model, SR2211 (20 mg/kg) inhibited the development of arthritis in a dose-dependent way [2]. References: |
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