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S202

Chemical Structure : S202

CAS No.: 2169248-42-2

S202 (CGT inhibitor S202)

Catalog No.: PC-38767Not For Human Use, Lab Use Only.

S202 is a potent, selective and brain-penetrant small molecule inhibitor of ceramide galactosyltransferase (CGT) with IC50 of 15 nM in the cell-lysate assays and 3.6 nM in intact-cell assays.

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    Biological Activity

    S202 is a potent, selective and brain-penetrant small molecule inhibitor of ceramide galactosyltransferase (CGT) with IC50 of 15 nM in the cell-lysate assays and 3.6 nM in intact-cell assays.
    S202 exhibits minimal to no activity toward other enzymes that act on related glycosphingolipids.
    S202 preferentially reduces non-hydroxy-GalCer synthesis in vivo.
    S202 (0-1.5 mg/kg) extends survival and reduces psychosine levels in a krabbe disease (KD) mouse model, causes a dose-dependent reduction in non-hydroxy-GalCer without reducing 2-hydroxy-GalCer in the brain.
    S202 (0.15 mg/kg, i.p. three times per week) improves histological and immunological markers in Twitcher mice.
    S202 treatment reduces non-hydroxy-sulfatides and lysosulfatide in an MLD mouse model.

    Physicochemical Properties

    M.Wt 586.203
    Formula C23H17Br2F3N2O3
    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

    (5R)-1,3-bis(4-bromophenyl)-4-hydroxy-5-methyl-4-(3-(trifluoromethoxy)phenyl)imidazolidin-2-one

    References

    1. Michael C Babcock, et al. Sci Rep. 2021 Jul 14;11(1):14486.

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