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Halofuginol

Chemical Structure : Halofuginol

CAS No.: 1363630-89-0

Halofuginol (MAZ1805)

Catalog No.: PC-49608Not For Human Use, Lab Use Only.

Halofuginol (MAZ1805) is a halofuginone analog targeting the Plasmodium falciparum prolyl-tRNA synthetase (PfcPRS, Ki=71.1 nM), is highly active against both liver and asexual blood stages of the malaria parasite (EC50=5.8 nM, P. falciparum 3D7 parasite strain).

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    Biological Activity

    Halofuginol (MAZ1805) is a halofuginone analog targeting the Plasmodium falciparum prolyl-tRNA synthetase (PfcPRS, Ki=71.1 nM), is highly active against both liver and asexual blood stages of the malaria parasite (EC50=5.8 nM, P. falciparum 3D7 parasite strain).
    Halofuginol is approximately 65 times more selective for P. falciparum than primary mouse embryonic fibroblasts.
    Halofuginol has similar activity (EC50=14 nM) to halofuginone (EC50 = 17 nM) in the in vitro P. berghei ANKA liver stage model.
    Halofuginol (5 mg/kg, i.p. or 10 mg/kg p.o) is active against the asexual erythrocytic and liver stages of the malaria parasite in P. berghei sporozoite challenge model, reduces parasite burden by more than 95%.

    Physicochemical Properties

    M.Wt 416.7
    Formula C16H19BrClN3O3
    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

    7-bromo-6-chloro-3-((S)-2-hydroxy-3-((2R,3S)-3-hydroxypiperidin-2-yl)propyl)quinazolin-4(3H)-one

    References

    1. Jonathan D Herman, et al. Sci Transl Med. 2015 May 20;7(288):288ra77.

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