RORγt Inverse agonist 6

RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the treatment of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> ROR

RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in a mouse pharmacodynamics model[1]. RORγt Inverse agonist 6 (compound 43) exhibits improved drug exposure (mouse AUC: 1289 ng•h/mL at 1 mg/kg, po)[1]. RORγt Inverse agonist 6 (compound 43, 30 mg/kg, po, b.i.d) inhibits the expression level of IL-17A by 59% compared to the vehicle after the oral administration at the tested dose[1]. Animal Model: Mice[1]. Dosage: 30 mg/kg. Administration: Orally twice: at 30 min before and 8 h after IL-23 administration. Result: Inhibited the expression level of IL-17A by 59% compared to the vehicle after the oral administration at the tested dose.

[1]. Sato A, et al. Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists. ChemMedChem. 2019 Oct 28.