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

Chemical Structure : GSK256066

CAS No.: 801312-28-7

GSK256066 (GSK 256066)

货号: PC-61617Not For Human Use, Lab Use Only.

GSK256066 is a highly potent, selective PDE4B inhibitor with pIC50 of 11.1, apparent IC50 of 3.2 pM, inhibits PDE4 isoforms A-D with equal affinity.

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5 mg ¥780 In stock
10 mg ¥1180 In stock
25 mg ¥2180 In stock
50 mg ¥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK256066 is a highly potent, selective PDE4B inhibitor with pIC50 of 11.1, apparent IC50 of 3.2 pM, inhibits PDE4 isoforms A-D with equal affinity.
GSK256066 displays >1,000-fold selectivity over PDE1, 2, 3, 5, 6, and 7.
GSK256066 inhibits LPS induced production of TNF-alpha from isolated human peripheral blood mononuclear cells with pIC50 of 11.1.
GSK256066 inhibits LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.
GSK256066 shows exceptional potency in vitro and in vivo for treatment for COPD and asthma.

物理化学性质&存储条件

分子量 518.588
分子式 C27H26N4O5S
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

6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

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. Singh D, et al. Respir Res. 2010 Mar 1;11:26.

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

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