PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity[1]. IC50: 4.1 nM (RORC2)[1]
PF-06747711 (Compound 66) reduces IL-17 production by human Th17 cells with an IC50 of 9.5 nM[1].
PF-06747711 (10, 30, and 100 mg/kg, p.o., daily over 5 days) inhibits ear swelling in a dose-dependent manner in mice[1]. Animal Model: 8-10 week old female Balb/c mice[1]
[1]. Schnute ME, et al. Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist. J Med Chem. 2018 Sep 9.