| CAS: | 801312-28-7 | |||
| 分子式: | C27H26N4O5S | |||
| 分子量: | 518.58 | |||
| 中文名称: |
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| 英文名称: |
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| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | 详情 | ||||||||||||||||||||||
| G792443 | MACKLIN | GSK-256066 | 10mM in DMSO | 2586元/1ml; | 展开 | ||||||||||||||||||||||
储存：-20°C | |||||||||||||||||||||||||||
| G873396 | MACKLIN | GSK-256066 | 98% | 520元/1mg; | 展开 | ||||||||||||||||||||||
储存：-20℃ 状态：浅黄色到黄色固体 | |||||||||||||||||||||||||||
| SML2102 | Sigma-Aldrich | GSK256066 | 974.06元/5 MG; 3926.75元/25 MG; | 展开 | |||||||||||||||||||||||
产品说明 生化/生理作用 GSK256066 is a reversible and cAMP-competitive phosphodiesterase 4 (PDE4) inhibitor that targets all PDE4 subtypes with high affinity (IC50 = 53.7 pM against 2 nM [3H]-rolipram for binding HRBS in rat brain cytosol), potency and selectivity (pIC50 ≥11.31/11.5/11.42/11.94 against PDE4A/B/C/D vs. pIC50 = 5.73/5.92/5.93/5.39/5.28/8.11 against PDE1/2/3/5/6/7 by SPA assays). GSK256066 effectively inhibits LPS-induced TNFα production from human whole blood and isolated PBMCs (pIC50 = 126 and 10 pM, respectively) in vitro and acute pulmonary neutrophilia in rats in vivo (ED50 = 1.1 μg/kg, administered intratracheally 2 hrs priror to LPS). GSK256066 is shown to be more potent than Cilomilast (SB-207499) and Roflumilast in both cell-free and cell-based assays. 基本信息
产品性质
安全信息
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