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Antimalarial agent 52 is an orally effective synthetic inhibitor of malaria pigment (β-hematin), with an IC50 of 6.6 μM. In vitro, it exhibits antimalarial activity against Plasmodium falciparum strains Pf3D7 and PfDd2, and Plasmodium knowlesi, with IC50 values of 6.1, 6.4, and 3.3 nM, respectively. It remains potent against multidrug-resistant strains and demonstrates significant efficacy in a Plasmodium berghei (P. berghei) mouse model.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | Antimalarial agent 52 is an orally effective synthetic inhibitor of malaria pigment (β-hematin), with an IC50 of 6.6 μM. In vitro, it exhibits antimalarial activity against Plasmodium falciparum strains Pf3D7 and PfDd2, and Plasmodium knowlesi, with IC50 values of 6.1, 6.4, and 3.3 nM, respectively. It remains potent against multidrug-resistant strains and demonstrates significant efficacy in a Plasmodium berghei (P. berghei) mouse model. |
| In vitro | Antimalarial agent 52 (Compound 7d) exhibits antiplasmodial activity against isolates from malaria patients and resistant mutant strains, with IC50 values of 4-16 nM and 8-15 nM, respectively. It is not metabolized by human liver microsomes, demonstrates high plasma stability, and shows improved cardiac safety. |
| In vivo | Compound 7d, referred to as Antimalarial agent 52, achieved a 100% cure rate at doses of 30 and 50 mg/kg in a P. berghei mouse model. The compound was administered orally at doses ranging from 3 to 50 mg/kg, with treatments given at 4, 24, 48, and 72 hours post-infection. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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