1359164-11-6

1359164-11-6结构式

中文名	SR2211
英文名	sr 2211
中文别名	1,1,1,3,3,3-六氟-2-(2-氟-4'-((4-(吡啶-4-基甲基)哌嗪-1-基)甲基)-[1,1'-联苯]-4-基)丙-2-醇 2-氟-4′-[[4-(4-吡啶基甲基)-1-哌嗪基]甲基]-Α,Α-双(三氟甲基)[1,1′-联苯]-4-甲醇 2-FLUORO-4'-[[4-(4-PYRIDINYLMETHYL)-1-PIPERAZINYL]METHYL]-伪,伪-BIS(TRIFLUOROMETHYL)-[1,1'-BIPHENYL]-4-METHANOL
英文别名	SR-2211,SR2211 [1,1'-Biphenyl]-4-methanol, 2-fluoro-4'-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl) 2-Fluoro-4'-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-a,a-bis(trifluoromethyl)-[1,1'-biphenyl]-4-methanol 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 1,1,1,3,3,3-Hexafluoro-2-(2-fluoro-4'-{[4-(4-pyridinylmethyl)-1-piperazinyl]methyl}-4-biphenylyl)-2-propanol RORγ Inverse Agonist, SR2211 2-Fluoro-4′-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-[1,1′-biphenyl]-4-methanol SR-2211 2-Fluoro-4'-[[4-(4-pyridinylMethyl)-1-piperazinyl]Methyl]-α,α-bis(trifluoroMethyl)-[1,1'-biphenyl]-4-Methanol SR2211, 10 mM in DMSO

描述	SR2211 是 RORγ 有效的,选择性合成调节剂,可作为反向激动剂发挥功能,其 Ki 值为 105 nM,IC50 值为 ~320 nM。
相关类别	信号通路 >> 代谢酶/蛋白酶 >> ROR 研究领域 >> 炎症/免疫
靶点	IC50: ~320 nM (RORγ), Ki: 105 nM (RORγ)[1][2].
体外研究	与地高辛相比,用SR2211处理EL4在更大程度上抑制了Il17基因的表达。类似地,如先前报道的,SR2211和地高辛显着抑制IL-23受体(Il23r)的表达。与载体处理的细胞相比,用SR2211以及对照地高辛处理EL-4细胞导致IL-17细胞内染色的显着抑制[1]。
参考文献	[1]. Kumar N, et al. Identification of SR2211: a potent synthetic RORγ-selective modulator. ACS Chem Biol. 2012 Apr 20;7(4):672-7. [2]. Song Y, et al. Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new RORγ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation. Eur J Med Chem. 2016 Jun 30;116:13-26.