| 应用 |
A highly potent and selective inhibitor of phosphodiesterase 4 |
| 产品介绍 |
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。 |
| 生化机理 |
GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity. |
| 别名 |
GSK-256066;GSK 256066; 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;GSK-256066;GSK 256066; 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide |
