GSK256066 is a highly potent, selective PDE4B inhibitor with pIC50 of 11.1, apparent IC50 of 3.2 pM, inhibits PDE4 isoforms A-D with equal affinity.
GSK256066 displays >1,000-fold selectivity over PDE1, 2, 3, 5, 6, and 7.
GSK256066 inhibits LPS induced production of TNF-alpha from isolated human peripheral blood mononuclear cells with pIC50 of 11.1.
GSK256066 inhibits LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.
GSK256066 shows exceptional potency in vitro and in vivo for treatment for COPD and asthma.
