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.
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- Formule: C24H17BrClF5N2O
- Masse moléculaire:559.75
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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.
| 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 |
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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Masse moléculaire 559.75
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antimalarial agent 52 Related Classifications
HY-178147 Related Classifications
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