| Bioactivity | 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[1]. | ||||||||||||
| Invitro | GSK256066 is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration[1]. GSK256066 is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7[1].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)[1].GSK256066 inhibits TNF-α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM[1]. | ||||||||||||
| In Vivo | GSK256066 (10 μg/kg; i.t.) causes significant inhibition of LPS-induced pulmonary neutrophilia[2].GSK256066 also inhibits LPS-induced increases in exhaled nitric oxide (ED50=92 μg/kg)[2].GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg)[2]. Animal Model: | ||||||||||||
| Name | GSK256066 | ||||||||||||
| CAS | 801312-28-7 | ||||||||||||
| Formula | C27H26N4O5S | ||||||||||||
| Molar Mass | 518.58 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
GSK256066
CAS: 801312-28-7 F: C27H26N4O5S W: 518.58
GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK25
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This product is for research use only, not for human use. We do not sell to patients.