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GSK256066

品牌
Sigma-Aldrich
CAS
801312-28-7
货号
SML2102
包装型号
规格纯度
价格
974.06 *本价格含增值税费
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半岛bd体育手机客户端 名称:
801312-28-7
GSK256066
GSK-256066
GSK 256066
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide
6-({3-[(Dimethylamino)carbonyl]phenyl}sulfonyl)-8-methyl-4-{[3-(methoxy)phenyl]amino}-3-quinolinecarboxamide
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 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 vitroand acute pulmonary neutrophilia in ratsin 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

经验(实验)分子式 C27H26N4O5S
分子量 518.58
MDL编号 MFCD18206923

半岛bd体育手机客户端 性质

测定 ≥97% (HPLC)
形式 powder
颜色 white to beige
溶解性 DMSO: 2 mg/mL, clear
储存温度 ?20℃

安全信息

储存分类代码 13 - Non Combustible Solids
WGK WGK 3

Sigma-Aldrich

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