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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-γ-secretase-PF-06648671
PF-06648671

Chemical Structure : PF-06648671

CAS No.: 1587727-31-8

PF-06648671 (PF6648671)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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).

    物理化学性质&存储条件

    分子量 538.928
    分子式 C25H23ClF4N4O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    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)-

    参考文献

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

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