6-[[3-[(二甲基氨基)羰基]苯基]磺酰]-4-[(3-甲氧基苯基)氨基]-8-甲基-3-喹啉甲酰胺

GSK256066是PDE4B抑制剂,IC50为3.2 pM,与A-D各亚型亲和力相同,比对PDE1/2/3/5/6和PDE7的抑制性高380000倍和2500倍。

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 炎症/免疫

[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]. Woodrow MD, et al. Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration. Bioorg Med Chem Lett, 2009, 19(17), 5261-5265.

[3]. 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.

3-异丁基-1-甲基黄嘌呤 | 咯利普兰 | PF-04957325 | 克立硼罗 | GLPG1690 | Bay 60-7550 | 淫羊藿苷 | 异丁司特 | 4-[3-氧代-3-(2-氧代-2,3-二氢苯并恶唑-6-基)丙基]哌嗪-1-羧酸 3,5-二氯苄酯 | TAK-063 | 双嘧达莫 | 西洛他唑 | 他达那非 | 己酮可可碱 | 西洛司特