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。
| 生物活性 | GSK256066 is a selective and high-affinityphosphodiesterase4 (PDE4)inhibitor, with anIC50of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease[1]. |
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体外研究
(In Vitro) | 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 IC50of 0.01 nM[1].
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体内研究
(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: | Male Brown Norway rats (180-200 g)[2] | | Dosage: | 10 μg/kg | | Administration: | Intratracheal injection; before (36 hours, 24 hours, 18 hours, 12 hours, 6 hours, and 2 hours) and after (0 hour, 2 hours) LPS challenge | | Result: | Inhibited the LPS-induced pulmonary neutrophilia. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(48.21 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.9283 mL | 9.6417 mL | 19.2834 mL | | 5 mM | 0.3857 mL | 1.9283 mL | 3.8567 mL | | 10 mM | 0.1928 mL | 0.9642 mL | 1.9283 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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