AA6216 (AA 6216) is novel potent, selective PDE4 inhibitor with IC50 of 0.63 nM.
AA6216 showed stronger inhibitory effects against PDE4 than other PDE family members.
AA6216 potently inhibits cytokine production (TNF-α,IL-12p40, IL-4, and IL-13, IC50s=2.2-7.9 nM) by PBMCs stimulated with PHA.
AA6216 inhibited the production of TGF-β1 by a human monocytic cell line THP-1, AA6216 dose-dependently reduced the production of TNF-α by alveolar macrophages from patients with IPF.
AA6216 demonstrated anti-fibrotic potency on mouse model of bleomycin-induced lung fibrosis.
