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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-GSK256066 trifluoroacetate
GSK256066 trifluoroacetate

Chemical Structure : GSK256066 trifluoroacetate

CAS No.: 1415560-64-3

GSK256066 trifluoroacetate (GSK-256066)

货号: PC-45952Not For Human Use, Lab Use Only.

GSK256066 trifluoroacetate is a potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK256066 trifluoroacetate is a potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively.
GSK256066 displays >380,000-fold selectivity over PDE1/23/5/6/7.
GSK256066 inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM.
GSK256066 inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rat.

物理化学性质&存储条件

分子量 632.6075
分子式 C29H27F3N4O7S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-, 2,2,2-trifluoroacetate (1:1)

参考文献

1. Woodrow MD, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5261-5.

2. Tralau-Stewart CJ, et al. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54.

3. Nials AT, et al. J Pharmacol Exp Ther. 2011 Apr;337(1):137-44.

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