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Referencia número: 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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No. CAS: 2770244-63-6
Fòrmula: C₂₆H₂₉ClN₄O₂
Peso molecular:464.99

Almacenamiento:

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

Antimalarial agent 64 Chemical Structure

No. CAS: 2770244-63-6

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Use of MCE Products

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

Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
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Actividad biológica

Descripciòn

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Cellular Effect

Cell Line	Type	Value	Description	References
HT-1080	IC₅₀	6.09 μM Compound: 12126038	Anticancer activity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay Anticancer activity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay	[PMID: 36208544]
SH-SY5Y	IC₅₀	3.41 μM Compound: 12126038	Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay	[PMID: 36208544]
SK-N-AS	IC₅₀	5.4 μM Compound: 12126038	Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay	[PMID: 36208544]

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

No. CAS 2770244-63-6
Peso molecular 464.99
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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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Help & FAQs

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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