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WM382

Chemical Structure : WM382

CAS No.: 2606990-92-3

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WM382 (WM-382)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 504.63
    分子式 C29H36N4O4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

    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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