1854901-94-2

TAK-828F is a potent and selective orally available RORγt inverse agonist. TAK-828F showed Binding IC50 = 1.9 nM; Reporter gene IC50=6.1 nM; logD=3.53; LLE (reporter gene)=4.68. TAK-828F inhibited IL-17 production from mouse splenocytes and human peripheral blood mononuclear cells dose-dependently at concentrations of 0.01-10?μM without affecting the production of IFN-γ. TAK-828F may provide a novel therapeutic option to treat immune diseases by inhibiting Th17 and Th1/17 cells' differentiation and improving imbalance between Th17 and Treg cells.

TAK-828F 是一种口服有效的选择性视黄酸受体相关孤儿受体 γt (RORγt) 反向激动剂 (结合 IC50=1.9 nM，报告基因 IC50=6.1nM)。TAK-828F 具有优异的 ROR 亚型选择性 (对 RORγt 的选择性比对人 RORα 和 RORβ 高 5000 多倍)。