1677668-27-7
1677668-27-7 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15404 英文別名
GNE-6468Benzoic acid, 4-[6-(2-chloro-6-cyclopropylbenzoyl)imidazo[1,5-a]pyrimidin-8-yl]-2-hydroxy-
物理化學(xué)性質(zhì)
密度1.55±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 5 mg/mL (11.52 mM)
酸度系數(shù)(pKa)2.35±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
應(yīng)用領(lǐng)域
用途一
GNE-6468 is a potent and selective RORc inverse agonist. GNE-6468 displayed >300-fold selectivity for RORc over the other ROR family members, PPARγ, and NRs in our cellular selectivity panel. The favorable potency, selectivity, and physiochemical properties of GNE-6468, in addition to its potent suppression of IL-17 production in human primary cells, support its use as chemical biology tools to further explore the role of RORc in human biology. The nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory cytokine interleukin-17.常見問題列表
概述
GNE-6468 是一個有效且有選擇性的 RORγ (RORc) 反向激動劑，EC50 值為 2 nM。GNE-6468 抑制 PBMC 中 IL-17 的 EC50 值為 30 nM。