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PF-06648671

Chemical Structure : PF-06648671

CAS No.: 1587727-31-8

PF-06648671 (PF6648671)

Catalog No.: PC-61830Not For Human Use, Lab Use Only.

PF-06648671 (PF6648671) is a potent, selective and oral γ-secretase modulator (GSM), reduces Aβ42 (IC50=9.8 nM) and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro.

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    Biological Activity

    PF-06648671 (PF6648671) is a potent, selective and oral γ-secretase modulator (GSM), reduces Aβ42 (IC50=9.8 nM) and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro.
    PF-06648671 exhibits excellent Aβ42-lowering activity in vivo with rat brain Aβ42 IC25 value of 3.4 nM.
    PF-06648671 shows good selectivity over Notch (Notch intracellular domain, NICD) (IC50>15.8 uM).
    PF-06648671 has favorable brain availability in rodent, which translated into excellent central exposure in human and robust reduction of amyloid β (Aβ) 42 in cerebrospinal fluid (CSF).

    Physicochemical Properties

    M.Wt 538.928
    Formula C25H23ClF4N4O3
    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

    2H-Pyrido[1,2-a]pyrazine-1,6-dione, 2-[(1S)-1-[(2S,5R)-5-[4-chloro-5-fluoro-2-(trifluoromethyl)phenyl]tetrahydro-2-furanyl]ethyl]-3,4-dihydro-7-(4-methyl-1H-imidazol-1-yl)-

    References

    1, Pettersson M, et al. J Med Chem. 2024 Jun 7. doi: 10.1021/acs.jmedchem.4c00580.

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