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GLPG0259

Chemical Structure : GLPG0259

CAS No.: 959754-85-9

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GLPG0259 (GLPG-0259)

Catalog No.: PC-24763Not For Human Use, Lab Use Only.

GLPG0259 is a potent, specific, ATP-competitive and orally bioavailable mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5, PRAK, MK5) inhibitor.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GLPG0259 is a potent, specific, ATP-competitive and orally bioavailable mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5, PRAK, MK5) inhibitor.
GLPG0259 reduces the release of several mediators of inflammation and bone degradation, such as MMP1, MMP13, TNF, and IL6.
GLPG0259 reduces paw inflammation as well as bone destruction in the mouse collagen-induced arthritis (CIA) model of human RA at a dose of 1 mg/kg and higher.

Physicochemical Properties

M.Wt 460.54
Formula C24H28N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(8-((4-(4-(tert-Butyl)piperazin-1-yl)phenyl)amino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-2-carboxamide

References

1. Namour F, et al. Drugs R D. 2012 Sep 1;12(3):141-63.

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