RORγt Inverse agonist 6

Biological Activity

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

References

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