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Antimalarial agent 25, a derivative of 1,4-naphthoquinones, demonstrates oral activity and is effective against malaria. It exhibits cytotoxic properties specifically targeting P. falciparum and effectively inhibits parasitemia induced by P. burghei in vivo [1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks |
Description | Antimalarial agent 25, a derivative of 1,4-naphthoquinones, demonstrates oral activity and is effective against malaria. It exhibits cytotoxic properties specifically targeting P. falciparum and effectively inhibits parasitemia induced by P. burghei in vivo [1]. |
In vitro | Antimalarial agent 25 (compound 8) exhibits an IC₅₀ of 4.2 μM against P. falciparum, while demonstrating CC₅₀ values of 289.2 μM for HepG2 cells and 400.6 μM for Vero cells [1]. In uninfected human red blood cells, concentrations ranging from 15.62 to 250 μM show hemolytic activity below 40% when treated for 2 hours [1]. At concentrations of 30 to 0.411 μg/mL over 48 hours, this agent causes substantial cytoplasmic degradation and loss of membrane integrity in the W2 strain of P. falciparum [1]. Cell viability assays indicate that the W2 strain (chloroquine-resistant) displays significant morphological changes, including dense cytoplasm with possible undefined organelles in a degenerating stage and potentially deteriorated food vacuoles [1]. |
In vivo | Antimalarial agent 25, administered orally at a dose of 30 mg/kg four times daily, enhances antimalarial activity against Plasmodium berghei in mice. In a single 300 mg/kg oral dose, this agent does not cause notable pathological changes or histopathological damage in female mice. In a model using mice infected with Plasmodium berghei ANKA, the treatment reduced parasitemia by 33% on the seventh day post-treatment. |
Molecular Weight | 374.39 |
Formula | C21H18N4O3 |
Cas No. | 2944456-41-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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