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GSK256066

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Chemical Structure| 801312-28-7 同义名 : -
CAS号 : 801312-28-7
货号 : A541549
分子式 : C27H26N4O5S
纯度 : 98+%
分子量 : 518.584
MDL号 : MFCD18206923
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(48.21 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PDE4

    PDE4B, IC50:3.2 pM
描述 Phosphodiesterases (PDEs) are a class of enzymes that hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) which are composed of 11 different families and each family contains different subtypes[3]. GSK256066 is a selective PDE4B inhibitor with IC50 of 3.2 pM. Consistent with its potency, GSK256066 inhibited tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 and by LPS-stimulated whole blood with 126 pM IC50[4]. When administered intratracheally to rats, GSK256066 inhibited LPS-induced pulmonary neutrophilia with ED50 values of 1.1 μg/kg (aqueous suspension) and 2.9 μg/kg (dry powder formulation) and was more potent than an aqueous suspension of the corticosteroid fluticasone propionate (ED50 9.3 μg/kg)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.64mL

1.93mL

0.96mL

19.28mL

3.86mL

1.93mL
参考文献

[1]Tralau-Stewart CJ, Williamson RA, 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 Apr;337(1):145-54.

[2]Woodrow MD, Ballantine SP, et al. Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5261-5.

[3]Peng T, Gong J, Jin Y, et al. Inhibitors of phosphodiesterase as cancer therapeutics. Eur J Med Chem. 2018;150:742–756.

[4]Tralau-Stewart CJ, Williamson RA, Nials AT, 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.