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GLPG-0634

GLPG-0634 is a triazolopyridine that inhibits JAK1; it exhibits anti-inflammatory and immunomodulatory activities. GLPG-0634 prevents release of inflammatory cytokines and is currently under investigation as a potential treatment for rheumatoid arthritis and Crohn’s disease.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18927621

Cas No.

1206161-97-8

Purity

≥98%

Formula

C21H23N5O3S

Formula Wt.

425.50

IUPAC Name

N-(5-{4-[(1,1-Dioxido-4-thiomorpholinyl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide

Synonym

GLPG0634, Filgotinib

Appearance

White Crystal Powder

Namour F, Diderichsen PM, Cox E, et al. Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection. Clin Pharmacokinet. 2015 Feb 14. [Epub ahead of print]. PMID: 25681059.

Menet CJ, Fletcher SR, Van Lommen G, et al. Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem. 2014 Nov 26;57(22):9323-42. PMID: 25369270.

Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. PMID: 24818516.

CP690550 citrate