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NYX-PCSK9i

Chemical Structure : NYX-PCSK9i

CAS No.: 2794203-47-5

NYX-PCSK9i

Catalog No.: PC-49372Not For Human Use, Lab Use Only.

NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of PCSK9, inhibits PCSK9-LDLR interaction with IC50 of 323 nM in in vitro biochemical binding assays.

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    Biological Activity

    NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of PCSK9, inhibits PCSK9-LDLR interaction with IC50 of 323 nM in in vitro biochemical binding assays.
    NYX-PCSK9i (30 and 50 mg/kg) demonstrates significant cholesterol-lowering properties in APOE*3-Leiden.CETP hyperlipidemic mice, significantly reduces plasma total cholesterol and elevates plasma total PCSK9 levels in a dose-dependent fashion.
    NYX-PCSK9i enhances the efficacy of atorvastatin in lowering plasma total cholesterol levels in female APOE*3-Leiden.CETP mice.
    NYX-PCSK9i modulates the hepatic transcriptional activity of specific genes involved in cholesterol metabolism (Pcsk9, Ldlr, Srebf2 and Mttp).
    NYX-PCSK9i depletes hepatic cholesteryl ester levels and promotes faecal cholesterol elimination in female APOE*3-Leiden.CETP mice.

    Physicochemical Properties

    M.Wt 466.589
    Formula C28H30N6O
    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

    (S)-N-(3-((3-aminopiperidin-1-yl)methyl)-5-(4-methyl-1H-imidazol-1-yl)phenyl)-4-phenylpicolinamide

    References

    1. Suchowerska AK, et al. J Lipid Res. 2022 Oct 6:100293.

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