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Antimalarial agent 52

Catalog No. T213267 Copy Product Info
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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.

Antimalarial agent 52

Copy Product Info
🥰Excellent
Catalog No. T213267

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.

Antimalarial agent 52
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
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.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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