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SPL-707

Chemical Structure : SPL-707

CAS No.: 2195361-33-0

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SPL-707 (SPL707)

Catalog No.: PC-62535Not For Human Use, Lab Use Only.

SPL-707 (SPL707) is the first selective, orally active signal peptide peptidase-like 2a (SPPL2a) inhibitor with IC50 of 77 nM, shows 25-fold selectivity over γ-secretase and SPP.

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    Biological Activity

    SPL-707 (SPL707) is the first selective, orally active signal peptide peptidase-like 2a (SPPL2a) inhibitor with IC50 of 77 nM, shows 25-fold selectivity over γ-secretase and SPP.
    SPL-707 significantly inhibits processing of the SPPL2a substrate CD74/p8 fragment in rodents at doses ≤10 mg/kg b.i.d. po., recapitulates the phenotype seen in Sppl2a knockout (ko) and ENU mutant mice after oral dosing of 40 for 11 days at ≥10 mg/kg b.i.d.

    Physicochemical Properties

    M.Wt 505.55
    Formula C27H28FN5O4
    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

    (S)-2-cyclopropyl-N1-((S)-5,11-dioxo-10,11-dihydro-1H,3H,5H-spiro[benzo[d]pyrazolo[1,2-a][1,2]diazepine-2,1'-cyclopropan]-10-yl)-N4-(5-fluoro-2-methylpyridin-3-yl)succinamide

    References

    1. Velcicky J, et al. J Med Chem. 2018 Feb 8;61(3):865-880.

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