| Identification | Back Directory | [Name]
GLPG0634 | [CAS]
1206101-20-3 | [Synonyms]
CS-1887
GLPG634 analog
GLPG0634 analogue
Filgotinib analog
GLPG0634 analog, Filgotinib analog
N-[5-[4-[(6-cyano-3-pyridinyl)Methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-cyclopropanecarboxaMide
N-(5-(4-((6-cyanopyridin-3-yl)methoxy)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide
Cyclopropanecarboxamide, N-[5-[4-[(6-cyano-3-pyridinyl)methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-
N-[5-[4-[(6-Cyano-3-pyridinyl)Methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl] cyclopropanecarboxaMide (GLPG0634)
N-[5-[4-[(6-Cyano-3-pyridinyl)methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-cyclopropanecarboxamide GLPG0634 analogue
GLPG0634 N-[5-[4-[(6-Cyano-3-pyridinyl)methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-cyclopropanecarboxamide | [Molecular Formula]
C23H18N6O2 | [MOL File]
1206101-20-3.mol | [Molecular Weight]
410.43 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light, stored under nitrogen | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥31.67 mg/mL in DMSO with gentle warming | [form ]
solid | [color ]
Light yellow to khaki |
| Hazard Information | Back Directory | [Uses]
N-[5-[4-[(6-Cyano-3-pyridinyl)methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide, is an orally-available, selective inhibitor of JAK1 (Janus kinase 1), used for the treatment of rheumatoid arthritis and potentially other inflammatory diseases. | [Biological Activity]
glpg0634 is a potent and selective inhibitor of jak1 with ic50 values of 10, 28, 810 and 116 nm for jak1, jak2, jak3 and tyk2, respectively [1].janus kinase 1 (jak1) is a member of the jak family and is a non-receptor tyrosine kinase. jaks play an important role in the immune system. jak1 is a potential target for the treatment of immune-inflammatory diseases [1].glpg0634 is a potent and selective jak1 inhibitor. glpg0634 inhibited jak1, jak2, jak3 and tyk2 with ic50 values of 10, 28, 810 and 116 nm, respectively. in cd4+ t cells, glpg0634 significantly reduced il-6-induced stat1 phosphorylation with ic50 value of 629 nm, which suggested the inhibition of jak1. in cd33+ t cells, glpg0634 reduced gm-csf-induced stat5 phosphorylation with ic50 value of 17.5 μm, suggesting the inhibition of jak2. glpg0634 inhibited the differentiation of th1 and th2 cells mediated by il-4 and il-12, respectively. also, glpg0634 inhibited th17 differentiation induced by tgf-β, il-23, il-6 and il-1β [1].in rats, glpg0634 significantly reduced the mrna levels of mx2, which were modulated by ifn-α-jak1/tyk2 signaling. in collagen-induced arthritis (cia) rat model, glpg0634 significantly reduced the infiltration of inflammatory cells and reduced the levels of il-6, ip-10, xcl1 and mcp-1 [1]. | [target]
JAK1 | [IC 50]
JAK1: <100 nM (IC50); JAK2: <100 nM (IC50); JAK3: <100 nM (IC50); Tyk2: <100 nM (IC50) | [storage]
4°C, protect from light, stored under nitrogen | [References]
[1]. van rompaey l, galien r, van der aar em, et al. preclinical characterization of glpg0634, a selective inhibitor of jak1, for the treatment of inflammatory diseases. j immunol, 2013, 191(7): 3568-3577. |
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