DC Chemicals · Product datasheet

Filgotinib(GLPG0634) — Datasheet

CAT. NO. DC7137

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ParameterValue
Chemical NameFilgotinib
CAS No.1206161-97-8
SynonymsFilgotinib;Filgotinib (GLPG0634);GLPG0634;GLPG-0634 (Filgotinib);GPLG0634;GPLG-0634;N-(5-(4-((1,1-Dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide;N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide;cyclopropanecarboxylic acid {5-[ 4-(1,1-dioxo-thiomorpholin-4-ylmethyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide;cyclopropanecarboxylic acid {5-[4-((1,1-dioxo-1-thimorpholin-4-yl)methyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide;GLPG-0634;N-[5-[4-[(1,1-Dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide;SYN1158;UNII-3XVL385Q0M;GLPG0634 （Filgotinib）;3XVL385Q0M;AK171369;Filgotinib [USAN:INN];GLPG 0634;N-(5-{4-[;Filgotinib(GLPG0634);G146034;N-(5-(4-((1,1-dioxido
FormulaC21H23N5O3S
M.Wt425.5
SMILESS1(C([H])([H])C([H])([H])N(C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])C2=C([H])C([H])=C([H])C3=NC(=NN23)N([H])C(C2([H])C([H])([H])C2([H])[H])=O)C([H])([H])C1([H])[H])(=O)=O
Purity98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

GLPG0634 is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

In Vitro

GLPG0634 dose-dependently inhibits the differentiation of Th2 cells mediated by IL-4, a cytokine that signals through JAK1 and JAK3. GLPG0634 also inhibits Th1 differentiation with similar potencies of 1 μM or lower[1]. GLPG0634 does not inhibit JAK2 homodimer-mediated signaling induced by EPO or PRL (IC50 > 10 μM)[2].

In Vivo

GLPG0634 (3, 10, 30 mg/kg, p.o.) dose-dependently prevents disease progression in the therapeutic rat CIA model. GLPG0634 (50 mg/kg, o.p.) protects bone and cartilage from degradation, effectively reduces infiltration of T cells (CD3+ cells) and macrophages (F4/80+ cells) in the paw, and decreases the serum levels of all cytokines and chemokines measured, including IL-6, IP-10, XCL1, and MCP-1[1]. GLPG0634 (0.1 and 0.3 mg/kg) shows efficacy in the rat CIA model[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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