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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-GSK356278
GSK356278

Chemical Structure : GSK356278

CAS No.: 720704-34-7

GSK356278 (GSK-356278)

货号: PC-60657Not For Human Use, Lab Use Only.

GSK356278 is a potent, selective, brain-penetrant and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with pIC50 of 8.8 (PDE4B).

规格 价格 库存 数量
10 mg ¥880 In stock
25 mg ¥1480 In stock
50 mg ¥2480 In stock
100 mg ¥3980 In stock
250 mg Get quote

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

生物&药学活性

GSK356278 is a potent, selective, brain-penetrant and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with pIC50 of 8.8 (PDE4B).
GSK356278 equally inhibits PDE4A and PDE4Dwith pIC50 of 8.6 and 8.7, exhibits >100-fold selectivity for PDE4B over the other 10 PDEs.
GSK356278 inhibits LPS-induced release of TNF-α in human whole blood with pIC50 of 7.6, demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in models of anxiety.

物理化学性质&存储条件

分子量 439.538
分子式 C21H25N7O2S
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

5-(5-((2,4-dimethylthiazol-5-yl)methyl)-1,3,4-oxadiazol-2-yl)-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine

参考文献

1. Rutter AR, et al. J Pharmacol Exp Ther. 2014 Jul;350(1):153-63.

2. van der Aart J, et al. J Cereb Blood Flow Metab. 2017 Jan 1:271678X17720868.

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