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BMS-869780

Chemical Structure : BMS-869780

CAS No.: 1235493-78-3

BMS-869780 (BMS869780)

Catalog No.: PC-62911Not For Human Use, Lab Use Only.

BMS-869780 is a potent γ-secretase modulator (GSM) that decreases Aβ1-42 (IC50=5.1 nM) and Aβ1-40 (IC50=25.1 nM) and increases Aβ1-37 and Aβ1-38 without inhibiting overall levels of Aβ peptides or other APP processing intermediates.

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    Biological Activity

    BMS-869780 is a potent γ-secretase modulator (GSM) that decreases Aβ1-42 (IC50=5.1 nM) and Aβ1-40 (IC50=25.1 nM) and increases Aβ1-37 and Aβ1-38 without inhibiting overall levels of Aβ peptides or other APP processing intermediates.
    BMS-869780 does not inhibit Notch processing by γ-secretase and loweres brain Aβ1-42 without evidence of Notch-related side effects in rats.
    BMS-869780 shows synergistic inhibition of Aβ combined with GSM-2.

    Physicochemical Properties

    M.Wt 452.918
    Formula C23H22ClFN6O
    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

    (9S)-N-[4-(4-Chloro-1H-imidazol-1-yl)-3-methoxyphenyl]-9-(4-fluorophenyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[1,5-a]azepin-2-amine

    References

    1. Toyn JH, et al. Int J Alzheimers Dis. 2014;2014:431858.

    2. Robertson AS, et al. Eur J Pharmacol. 2017 Oct 5;812:104-112.

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