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SPL-410

Chemical Structure : SPL-410

CAS No.: 2351886-00-3

SPL-410 (SPL410)

Catalog No.: PC-73009Not For Human Use, Lab Use Only.

SPL-410 (SPL410) is a highly potent, selective, orally active inhibitor SPPL2a (Signal Peptide Peptidase Like 2a) with IC50 of 9 nM.

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    Biological Activity

    SPL-410 (SPL410) is a highly potent, selective, orally active inhibitor SPPL2a (Signal Peptide Peptidase Like 2a) with IC50 of 9 nM.
    Both human and mouse SPPL2a was inhibited with high potency (IC50 of 0.004 μM and 0.005 μM) in high content imaging assay (HCA).
    SPL-410 is selective against closely related human aspartyl proteases such as SPP (0.65 μM) and γ-secretase (1.3 μM) as well as SPPL2b (0.27 μM in HCA)
    SPL-410 inhibited the processing of the endogenous substrate CD74/p8 NTF in IC50 of 0.15 μM in the mouse B cell line A20.
    SPL-410 caused accumulation of CD74/p8 NTF (10 mg/kg single p.o. dose) in mice, achieved a higher efficacy than LY-411575.

    Physicochemical Properties

    M.Wt 500.58
    Formula C24H31F3N2O4S
    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

    Benzenesulfonamide, N-[(2S,3S)-3-amino-2-hydroxy-3-[4-(trifluoromethoxy)phenyl]propyl]-N-cyclobutyl-4-(1,1-dimethylethyl)-

    References

    1. Velcicky J, et al. ACS Med Chem Lett. 2019 May 23;10(6):887-892.

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