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Art. -Nr.: HY-184182

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Antimalarial agent 64

Antimalarial agent 64 is an orally active acridine-based antimalarial derivative and also a rapid-acting inhibitor of hemozoin formation. Antimalarial agent 64 exhibits nanomolar inhibitory activity against field isolates of Plasmodium falciparum and Plasmodium vivax. Antimalarial agent 64 localizes near the digestive vacuole of Plasmodium. Antimalarial agent 64 can be used for the research of malaria.

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CAS. Nr.: 2770244-63-6
Formel: C₂₆H₂₉ClN₄O₂
Molecular Weight:464.99

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Antimalarial agent 64 Chemical Structure

CAS. Nr.: 2770244-63-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
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Biologische Aktivität

Beschreibung

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In Vitro

Antimalarial agent 64 (Compound 2d) potently inhibits Chloroquine (HY-17589A)-sensitive Plasmodium falciparum 3D7 strain growth with an IC₅₀ of 20 nM, has a CC₅₀ of 6 μM against HepG2 cells, and a selectivity index of 300^[1].
Antimalarial agent 64 retains potent antiplasmodial activity against Plasmodium falciparum K1, Dd2, and 3D7^R_MMV848 multidrug-resistant strains but shows cross-resistance with atovaquone in the TM90C6B strain^[1].
Antimalarial agent 64 potently inhibits ex vivo growth of Plasmodium falciparum (IC₅₀ = 39 nM) and Plasmodium vivax (IC₅₀ = 21 nM) field isolates from the Brazilian Amazon^[1].
Antimalarial agent 64 potently inhibits ring and trophozoite stages of Plasmodium falciparum 3D7 strain, with reduced activity against schizonts^[1].
Antimalarial agent 64 (10 μM) selectively accumulates near the digestive vacuole of Plasmodium falciparum-infected erythrocytes, with no uptake in uninfected red blood cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Antimalarial agent 64 (Compound 2d) (50 mg/kg/day; p.o.; once daily; 3 consecutive days post-infection) achieves 100% parasitemia reduction and 100% survival at 30 days in mice infected with P. berghei NK65^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

mice infected
with P. berghei NK65 strain
^[1]
Dosage:

50 mg/kg/day
Administration:

p.o.; once daily; 3 consecutive days post-infection
Result:

Achieved 100% reduction in parasitemia at days 5, 8, and 11 post-infection compared to untreated controls.
Showed 100% survival at 30 days post-infection, comparable to chloroquine-treated controls.

Chemical Information

CAS. Nr. 2770244-63-6
Molecular Weight 464.99
Formel C₂₆H₂₉ClN₄O₂
SMILES

COC1=CC2=C(C3=CC=C(C=C3N=C2C=C1)Cl)NC4=CC(CN(C)C)=C(C(CN(C)C)=C4)O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Maluf SEC, et al. Efficacy, Structure-Activity Relationship, and Mode of Action Studies of a New Generation of Acridine/Acridone-Based Antimalarials. ACS Infect Dis. 2026 Jun 12;12(6):1866-1883.
[Content Brief]

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
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- In Vivo
Chemical Information
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Antimalarial agent 64

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