Filgotinib-d4 (Synonyms: GLPG0634-d4) |
| Catalog No.GC46148 |
Filgotinib-d4(GLPG0634-d4)는 Filgotinib으로 표시된 중수소입니다. 필고티닙(GLPG0634)은 JAK1, JAK2, JAK3 및 TYK2에 대해 IC50이 각각 10nM, 28nM, 810nM 및 116nM인 선택적 JAK1 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2041095-50-3
Sample solution is provided at 25 µL, 10mM.
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Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib by GC- or LC-MS. Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).1 It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3 and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 μM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.
|1. Van Rompaey, L., Galien, R., van der Aar, E.M., et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J. Immunol. 191(7), 3568-3577 (2013).
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