A potent

GSK356278 – 50 mg

Brand:
Cayman
CAS:
720704-34-7
Storage:
-20
UN-No:
Non-Hazardous - /

GSK356278 is a potent, selective, and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with anxiolytic and cognition-improving effects.{55071} It is greater than 100-fold selective for PDE4A, -B, and -D (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively) over 10 other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels, and enzymes. It inhibits LPS-induced release of TNF-α in isolated human whole blood (IC50 = 23.1 nM) and reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg). GSK356278 (0.01-1 mg/kg) induces anxiolytic behavior in marmosets, and improves performance of non-human primates in an object retrieval test when administered at a dose of 1 mg/kg.  

 

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SKU: 30412 - 50 mg Category:

Description

A potent, selective, and orally bioavailable PDE4 inhibitor (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively); >100-fold selective for PDE4 over other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels and enzymes; inhibits LPS-induced release of TNF-α in human whole blood (IC50 = 23.1 nM); reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg); induces anxiolytic behavior in marmosets at 0.01-1 mg/kg; improves performance of non-human primates in an object retrieval test at 1 mg/kg

Formal name: 5-[5-[(2,4-dimethyl-5-thiazolyl)methyl]-1,3,4-oxadiazol-2-yl]-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine

Synonyms: 

Molecular weight: 439.5

CAS: 720704-34-7

Purity: ≥98%

Formulation: A crystalline solid

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