GSK256066 是一种选择性、高亲和力的 PDE4 抑制剂，抑制 PDE4B 的 IC₅₀ 值为 3.2 pM。GSK256066 被开发用于慢性阻塞性肺病的研究。

GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC 50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.

Solid

PDE4 3.2 pM (IC50)

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.
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 (ED 50 =92 μg/kg).
GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED 50 =0.4 μg/kg).
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. 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.
[2]. 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.

In Vitro: DMSO : 25 mg/mL (48.21 mM; ultrasonic and warming and heat to 60°C)配制储备液