GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC₅₀ of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.

GSK256066 is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration.
GSK256066 is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7.
GSK256066 inhibits PDE4 isoforms A-D with equal affinity (PDE4B: pIC₅₀≥ 11.5, PDE4A: pIC₅₀≥11.31, PDE4C: pIC₅₀≥11.42, PDE4D: pIC₅₀≥11.94).
GSK256066 inhibits TNF-α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC₅₀ of 0.01 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

GSK256066 (10 μg/kg; i.t.) causes significant inhibition of LPS-induced pulmonary neutrophilia.
GSK256066 also inhibits LPS-induced increases in exhaled nitric oxide (ED₅₀=92 μg/kg).
GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED₅₀=0.4 μg/kg).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

GSK256066 (10 μg/kg; i.t.) causes significant inhibition of LPS-induced pulmonary neutrophilia.
GSK256066 also inhibits LPS-induced increases in exhaled nitric oxide (ED₅₀=92 μg/kg).
GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED₅₀=0.4 μg/kg).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Tralau-Stewart CJ, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther, 2011, 337(1), 145-154.  [Content Brief]

  . Nials AT, et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther, 2011, 337(1), 137-144.  [Content Brief]