Tanimilast (CHF6001) is a novel, highly potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 0.026 nM.
CHF6001 inhibits PDE4 isoforms A-D with equal potency, 7- and 923-fold more potent than roflumilast and cilomilast, and displays >20,000-fold selectivity versus PDE4 compared with a panel of PDEs.
CHF6001 effectively inhibits (subnanomolar IC50 values) the release of TNF-α from human PBMCs, THP-1, and rodent macrophages.
CHF6001 inhibitsLPS-induced pulmonary neutrophilia (ED50=0.205 uM/kg) and leukocyte infiltration (ED50=0.188 uM/kg) in rats.
