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Ganaplacide

Chemical Structure : Ganaplacide

CAS No.: 1261113-96-5

Ganaplacide (KAF156;GNF-156)

Catalog No.: PC-61378Not For Human Use, Lab Use Only.

Ganaplacide (KAF156, GNF-156) is a novel antimalarial clinical candidate that shows blood schizonticidal activity with IC50 of 6-17.4 nM against P falciparum drug-sensitive and drug-resistant strains.

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    Biological Activity

    Ganaplacide (KAF156, GNF-156) is a novel antimalarial clinical candidate that shows blood schizonticidal activity with IC50 of 6-17.4 nM against P falciparum drug-sensitive and drug-resistant strains.
    KAF156 demonstrates potent therapeutic activity in mouse models of malaria with 50, 90, and 99% effective doses of 0.6, 0.9, and 1.4 mg/kg, respectively.
    KAF156 is completely protective as a single oral dose of 10 mg/kg in sporozoite challenge mouse model.
    KAF156 shows the potential to treat, prevent, and block the transmission of malaria.

    Physicochemical Properties

    M.Wt 411.457
    Formula C22H23F2N5O
    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

    2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]ethan-1-one

    References

    1. Kuhen KL, et al. Antimicrob Agents Chemother. 2014 Sep;58(9):5060-7.

    2. Leong FJ, et al. Antimicrob Agents Chemother. 2014 Nov;58(11):6437-43.

    3. Lim MY, et al. Nat Microbiol. 2016 Sep 19:16166.

    4. White NJ, et al. N Engl J Med. 2016 Sep 22;375(12):1152-60.

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