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    Filgotinib (GLPG-0634)
    Filgotinib (GLPG-0634)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0326
    CAS #: 1206161-97-8Purity ≥98%

    Description: Filgotinib (also known as GLPG0634) is a novel, potent and selective JAK1 (Janus kinase) inhibitor with potential anti-inflammatory activity. It inhibits JAK1, JAK2, JAK3, and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM, and 116 nM, respectively. It is currently being investigated for the treatment of rheumatoid arthritis (RA) and Crohn's disease. It is considered to be a promising drug candidate for treating autoimmune diseases by selectively inhibiting JAK1. In cellular assays, GLPG0634 is most potent in inhibiting the JAK1/JAK3/γc signaling induced by IL-2– and IL-4 as well as the JAK1/TYK2 type II receptor signaling induced by IFN-αB2. However, it shows lower potent to inhibit JAK2 homodimer–mediated signaling induced by EPO or PRL. In addition, GLPG0634 is found to inhibit the phosphorylation of STAT1 and STAT5 induced by cytokines.

    References: J Immunol. 2013 Oct 1;191(7):3568-77.

    Related CAS:1206101-20-3 (GLPG0634 analogue); 1206161-97-8; 1206101-20-3  

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    Molecular Weight (MW)425.50
    FormulaC21H23N5O3S
    CAS No.1206101-20-3 (GLPG0634 analogue); 1206161-97-8; 1206101-20-3;
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 85 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)4% DMSO+30% PEG 300+ddH2O: 3mg/mL 
    Synonyms

    PubChemSID 163643231; GLPG0634; GLPG 0634; GLPG-0634; Filgotinib

    Chemical Name: N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide.

    SMILES Code: O=C(C1CC1)NC2=NN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)C=C4)=CC=CC3=N2 


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    In Vitro

    In vitro activity: In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells.


    Kinase Assay: Recombinant JAK1, TYK2, JAK2, and JAK3 are used to develop activity assays in 50 mM HEPES (pH 7.5), 1 mM EGTA, 10 mM MgCl2, 2 mM DTT, and 0.01% Tween 20. The amount of JAK protein is determined per aliquot, maintaining initial velocity and linearity over time. The ATP concentration is equivalent to 4× the experimental Km value and the substrate concentration (ULight-conjugated JAK-1(Tyr1023) peptide) corresponds to the experimentally determined Km value. After 90 min incubation at room temperature (RT), the amount of phosphorylated substrate is measured by addition of 2 nM europium-anti-phosphotyrosine Ab and 10 mM EDTA in Lance detection buffer. Compound IC50 values are determined by preincubating the enzyme with compound at RT for 60 min, prior to the addition of ATP. 


    Cell Assay: 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.

    In VivoFollowing oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (∼100%). Filgotinib (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice. Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon.
    Animal modelIn the rat model of collagen-induced arthritis (CIA), oral administration of GLPG0634 shows a marked protection from bone damage at dose of 3 mg/kg. It reduces the infiltration of inflammatory cells significantly from 1 mg/kg onward
    Formulation & Dosage 30 mg/kg daily in Rats); 50 mg/kg twice daily in Mice
    ReferencesJ Immunol. 2013 Oct 1;191(7):3568-77.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Filgotinib (GLPG0634)

    GLPG0634 inhibits the differentiation of Th1, Th2, and Th17 cells. J Immunol.2013 Oct 1;191(7):3568-77.

    Filgotinib (GLPG0634)

    GLPG0634 dose-dependently prevents disease progression in the therapeutic rat CIA model. J Immunol. 2013 Oct 1;191(7):3568-77.

    Filgotinib (GLPG0634)

    GLPG0634 is efficacious in a mouse therapeutic CIA model. J Immunol. 2013 Oct 1;191(7):3568-77.


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