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GLPG4471

Chemical Structure : GLPG4471

CAS No.: 2499855-36-4

GLPG4471 (GLPG-4471)

Catalog No.: PC-25433Not For Human Use, Lab Use Only.

GLPG4471 (GLPG-4471) is a a potent and selective IRAK4 inhibitor with IC50 of 1.7 nM, potently inhibits CL097-induced TNFα in PBMCs with IC50 of 39.4 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    GLPG4471 (GLPG-4471) is a a potent and selective IRAK4 inhibitor with IC50 of 1.7 nM, potently inhibits CL097-induced TNFα in PBMCs with IC50 of 39.4 nM.
    GLPG4471 potently inhibits the CL097-induced secretion of TNFα and IFNα in human whole blood stimulated with IC50 of 17.1 and 28.0 nM respectively.
    GLPG4471 inhibits mouse IRAK4 with IC50 of 2.4 nM.
    GLPG4471 displays excellent kinome selectivity against a panel of 369 kinases at 1 uM.
    GLPG4471 (30  mg/kg, b.i.d, ora) lexhibited dose-dependent activity in vivo in the CIA mouse model of rheumatoid arthritis.

    Physicochemical Properties

    M.Wt 410.47
    Formula C22H26N4O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1-cyclopropyl-N-(2-(3-hydroxy-3-methylbutyl)-6-methoxypyrazolo[1,5-a]pyridin-5-yl)-2-oxo-1,2-dihydropyridine-3-carboxamide

    References

    1. Mammoliti O, et al. Bioorg Med Chem Lett. 2025 Aug 23:130386.

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