TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (IC50=1.9 nM, reporter gene IC50=6.1 nM).

RORγt, reporter gene IC50:6.1 nM , RORγt, binding IC50:1.9 nM

In mice with IL-23-induced cytokine expression model, TAK-828F (0.3, 1, and 3 mg/kg; orally administered; b.i.d.; 28 days; ) shows robust and dose-dependent inhibition of IL-17A expression with an ED80 of 0.5 mg/kg.