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WM382

Chemical Structure : WM382

CAS No.: 2606990-92-3

WM382 (WM-382)

Catalog No.: PC-49829Not For Human Use, Lab Use Only.

WM382 (WM-382) is a potent, specific dual inhibitor of the aspartic proteases Plasmepsin IX and X (PMIX and PMX) with IC50 of 0.06 nM (PMX), blocks multiple stages of the Plasmodium life cycle.

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    Biological Activity

    WM382 (WM-382) is a potent, specific dual inhibitor of the aspartic proteases Plasmepsin IX and X (PMIX and PMX) with IC50 of 0.06 nM (PMX), blocks multiple stages of the Plasmodium life cycle.
    WM382 displays no activity against the P. falciparum aspartic protease PMV (>300,000-fold).
    WM382 inhibits P. falciparum and P. knowlesi growth with EC50s of 0.6 nM and 0.2 nM, respectively.
    WM382 is not cross-resistant to other antimalarial drugs (chloroquine, mefloquine, artemisinin, and atovaquone).
    WM382 (2.5 nM) potently inhibited egress of merozoites from the erythrocyte.
    WM382 (20 mpk, orally administered twice daily (b.i.d. dosage)) suppresses P. berghei and P. falciparum infection infection in mice infected models.
    WM382 prevents transmission to mosquitoes and transition from liver to blood infection.

    Physicochemical Properties

    M.Wt 504.63
    Formula C29H36N4O4
    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

    (R)-4-(4,4-diethyl-2-imino-6-oxotetrahydropyrimidin-1(2H)-yl)-N-((S)-2,2-dimethylchroman-4-yl)chromane-6-carboxamide

    References

    1. de Lera Ruiz M, et al. ACS Med Chem Lett. 2022 Oct 12;13(11):1745-1754.

    2. Favuzza P, et al. Cell Host Microbe. 2020 Apr 8;27(4):642-658.e12.

    3. Hodder AN, et al. Structure. 2022 Jul 7;30(7):947-961.e6.

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