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ISM012-042

Chemical Structure : ISM012-042

CAS No.: 2924181-80-4

ISM012-042 (Garutadustat)

Catalog No.: PC-23633Not For Human Use, Lab Use Only.

Garutadustat (ISM012-042) is a potent, orally gut-restricted, selective PHD1 and PHD2 inhibitor with IC50 of 1.9 nM and 2.5 nM for PHD1 hydroxylase and PHD2 hydroxylase, respectively.

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    Biological Activity

    Garutadustat (ISM012-042) is a potent, orally gut-restricted, selective PHD1 and PHD2 inhibitor with IC50 of 1.9 nM and 2.5 nM for PHD1 hydroxylase and PHD2 hydroxylase, respectively.
    ISM012-042 exhibits gut-restricted pharmacokinetic (PK) properties, excellent activity and specificity against PHDs.
    ISM012-042 resolves colitis, restores intestinal barrier function and reprograms the colonic immune environment.
    ISM012-042 inhibited PHDs independently of extracellular iron levels and exerted anticolitis activity at markedly lower doses than SOC treatment mesalamine.
    ISM012-042 attenuated colitis by restoring intestinal barrier function and alleviating intestinal inflammation.

    Physicochemical Properties

    M.Wt 489.54
    Formula C25H27N7O4
    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

    tert-butyl 4-(6-(((6-cyanopyridin-3-yl)methyl)carbamoyl)-5-hydroxy-1,7-naphthyridin-2-yl)piperazine-1-carboxylate

    References

    1. Fu Y, et al. Nat Biotechnol. 2024 Dec 11. doi: 10.1038/s41587-024-02503-w.

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