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Filgotinib(GLPG0634)

  Cat. No.:  DC7137   Featured
Chemical Structure
1206161-97-8
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More than 5000 active chemicals with high quality for research!
Field of application
Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1206161-97-8
Chemical Name: Filgotinib
Synonyms: Filgotinib;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
SMILES: S1(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
Formula: C21H23N5O3S
M.Wt: 425.504
Purity: 98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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 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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC8736 Tofacitinib Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.
DC10779 PF-06651600 PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.
DC8168 Peficitinib（ASP015K,JNJ-54781532） Peficitinib(ASP015K,JNJ-54781532) is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats.
DC7137 Filgotinib(GLPG0634) Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease.
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