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MBX-4055

Chemical Structure : MBX-4055

CAS No.: 2807469-07-2

MBX-4055 (MBX4055)

Catalog No.: PC-49005Not For Human Use, Lab Use Only.

MBX-4055 is a potent and specific antimalarial compound with IC50 of 42 nM (P. falciparum growth inhibition), acts directly on plasmodial surface anion channel (PSAC, Target K0.5=21 nM) to quantitatively abolish parasite-induced permeability changes.

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    Biological Activity

    MBX-4055 is a potent and specific antimalarial compound with IC50 of 42 nM (P. falciparum growth inhibition), acts directly on plasmodial surface anion channel (PSAC, Target K0.5=21 nM) to quantitatively abolish parasite-induced permeability changes.
    MBX-4055 is active against divergent human parasite strains, with improved oral absorption with acceptable in vivo tolerability and pharmacokinetics.
    MBX-4055 is highly specific for the PSAC target without activity against a battery of human channels, enzymes and receptors, is refractory to acquired resistance during extended in vitro selection.

    Physicochemical Properties

    M.Wt 418.490
    Formula C17H18N6O3S2
    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

    6-(5-((4-(3-methylpyrazin-2-yl)piperazin-1-yl)sulfonyl)thiophen-2-yl)pyridazin-3(2H)-one

    References

    1. Michelle M Butler, et al. Mol Pharmacol. 2022 Jul 7;MOLPHARM-AR-2022-000549.

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