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S-181

Chemical Structure : S-181

CAS No.: 2270984-21-7

S-181 (S 181)

Catalog No.: PC-73111Not For Human Use, Lab Use Only.

S-181 (S 181) is a specific small-molecule activator (modulator) of β-glucocerebrosidase (GCase) with AC50 of 1.49 uM and a maximum activation of 780%.

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    Biological Activity

    S-181 (S 181) is a specific small-molecule activator (modulator) of β-glucocerebrosidase (GCase) with AC50 of 1.49 uM and a maximum activation of 780%.
    S-181 displays no effect in vitro enzyme activity of the lysosomal enzymes acid α-glucosidase and α-galactosidase A.
    S-181 (5 to 25 uM) is sufficient to increase wild-type GCase activity in iPSC-derived dopaminergic neurons.
    S-181 partially rescues pathogenic phenotypes in GBA-PD iPSC-derived dopaminergic neurons.
    S-181 lowers oxidized dopamine and α-synuclein in non-GBA1-linked PD patient iPSC-derived dopaminergic neurons.
    S-181 lowers lipid substrate and α-synuclein accumulation in wild-type (Gba1+/+) and Gba1D409V/+ mutant mice.

    Physicochemical Properties

    M.Wt 384.439
    Formula C23H20N4O2
    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

    N-[[(2S)-2,3-Dihydro-1,4-benzodioxin-2-yl]methyl]-N-methyl-2-(3-pyridinyl)-4-quinazolinamine

    References

    1. Burbulla LF, et al. Sci Transl Med. 2019 Oct 16;11(514). pii: eaau6870.

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