PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 μM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.In Vitro: PDE4B-IN-2 (compound 33) does not inhibit CYP1A2, CYP3A4, CYP2C9, and CYP2D (IC50>10 μM).
PDE4B-IN-2 inhibits LPS-induced TNF-aproduction in vitro from mouseperipheral blood mononuclear cell (PBMC; IC50=0.5 M).
In Vivo: PDE4B-IN-2 (compound 33; 2 mg/kg; po) has a Cmax of 8.7 μg/mL and an AUC of 52.3 μg?h/mL in mice.