RORγt inverse agonist 1 is a potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays.
RORγt inverse agonist 1 shows no inhibitory activity against the closely related nuclear hormone receptors RORα or RORβ.
RORγt inverse agonist 1 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.
