RORγt inverse agonist 22

RORγt inverse agonist 22 is a potent, subtype selective RORγt inverse agonist with binding IC50 of 18 nM, displays >192-fold selectivity over RORα and RORβ; exhibits cellular potency in RORγt reporter gene assays with IC50 of 13 nM, also shows >250-fold selectivity over a panel of 20 nuclear receptors; demonstrates in vivo potency to suppress the transcriptional activity of RORγt in a mouse PD model upon oral administration.

References 1. Shirai J, et al. Bioorg Med Chem. 2018 Jan 15;26(2):483-500. View Related Products by Target ROR