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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- 화학식: C24H17BrClF5N2O
- 분자량:559.75
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
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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분자량 559.75
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)