A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 drive
ROR agonist-1 is a potent and orally bioavailable the retinoic acid receptor-related orphan receptor C2 (RORC2) inverse agonist(inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5).
RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively).