Filgotinib-d<sub>4</sub>

Filgotinib-d4

CAT N°: 28875
Price:

From 460.00 391.00

Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib (Item No. 17669) by GC- or LC-MS. Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} 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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-cyclopropane-2,2,3,3-d4-carboxamide
  • Correlated keywords
    • GLPG 0634 GCMS LCMS deuterated deuterium JAK 1 3 Tyk FLT FLT3 FLT4 TBK IL6 interleukin STAT CD CD4
  • Product Overview:
    Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib (Item No. 17669) by GC- or LC-MS. Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} 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.

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