RORγt inhibitor 1

A potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays; shows no inhibitory activity against the closely related nuclear hormone receptors RORα or RORβ; attenuates expression of genes such as IL26, IL23R and CCR6 in primary human Th17 cells, attenuate the knee swelling response in an antigen-induced arthritis rat models and inhibits IL-17A cytokine production in ex vivo recall assays.

References 1. Guendisch U, et al. PLoS One. 2017 Nov 20;12(11):e0188391. 2. Hintermann S, et al. ChemMedChem. 2016 Dec 16;11(24):2640-2648. View Related Products by Target ROR