Antimalarial agent 52
Antimalarial agent 52 is an orally active formation of synthetic hemozoin (β-hematin) inhibitor with an IC50 of 6.6 μM. Antimalarial agent 52 exhibits in vitro antiplasmodial activity against P. falciparum Pf3D7, PfDd2 strains and P. knowlesi with IC50s of 6.1, 6.4 and 3.3 nM. Antimalarial agent 52 remain highly effective against multidrug-resistant strains and demonstrates curative activity in the P. berghei mouse model.
For research use only. We do not sell to patients.
- Formula: C24H17BrClF5N2O
- Molecular Weight:559.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
Description
In Vitro
Antimalarial agent 52 (Compound 7d) (48 h) exhibits antiplasmodial activity against field isolates from malaria patients and drug-resistant mutant strains with IC50s of 4-16 nM and 8-15 nM[1].
Antimalarial agent 52 is not metabolized by human liver microsomes, has high plasma stability and shows improved cardiac safety[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | AUC0-t | Brain-to-Plasma Ratio |
|---|---|---|---|---|---|---|
| Mice[1] | 50 mg/kg | p.o. | 2236.4 ng/mL | 49002 ng·h/mL | 4 h | 0.97 |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:P. berghei infection model established in female NMRI mice[1]
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Dosage:3, 10, 30 and 50 mg/kg
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Administration:Oral administration (p.o.), 4, 24, 48, 72 hours after infection for 4 doses
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Result:Showed significant dose-dependent antimalarial activity.
Chemical Information
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Molecular Weight 559.75
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Formula C24H17BrClF5N2O
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SMILES
N=C(NC1=CC=C(Br)C=C1)CC(C2=CC3=C(F)C=C(F)C=C3C4=CC(C(F)(F)F)=CC=C42)O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)