GSK 356278 ( GSK356278;GSK-356278 )

Catalog No. M15757 CAS No. 720704-34-7

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Product Name

GSK 356278
Note

Research use only, not for human use.
Brief Description

A potent, selective, brain-penetrant and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with pIC50 of 8.8 (PDE4B); equally inhibits PDE4A and PDE4Dwith pIC50 of 8.6 and 8.7.
Description

A potent, selective, brain-penetrant and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with pIC50 of 8.8 (PDE4B); equally inhibits PDE4A and PDE4Dwith pIC50 of 8.6 and 8.7, exhibits >100-fold selectivity for PDE4B over the other 10 PDEs; 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.Anxiety Phase 1 Clinical
Synonyms

GSK356278;GSK-356278
Pathway

Angiogenesis
Target

PDE
Recptor

PDE
Research Area

Neurological Disease
Indication

Anxiety

CAS Number

720704-34-7
Formula Weight

439.54
Molecular Formula

C21H25N7O2S
Purity

>98% (HPLC)
Solubility

——
SMILES

CCN1N=CC2=C(NC3CCOCC3)C(C4=NN=C(CC5=C(C)N=C(C)S5)O4)=CN=C21
Chemical Name

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

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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