Antimalarial agent 62
Antimalarial agent 62 is an orally active imidazopyridine-6-carboxamide antimalarial agent with a high resistance barrier. Antimalarial agent 62 kills trophozoite-stage Plasmodium ring forms, effectively clears dihydroartemisinin-induced dormant Plasmodium ring forms, and eliminates parasitemia in mice infected with Plasmodium yoelii. In AReBaR resistance omics screening, Antimalarial agent 62 is not affected by different target- and efflux-mediated resistance mutations and can withstand resistance selection. Antimalarial agent 62 has been applied to studies of malaria-related mechanisms.
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- Fòrmula: C22H19Cl4N5O
- Peso molecular:511.23
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
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Plasmodium |
| Species | Dose | Route | Cmax | Tmax | T1/2 (Elimination) | AUC0-24 | AUC0-inf | Vd | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 40 mg/kg | p.o. | 378 ng/mL | 5.3 h | 23.1 h | 6030 ng·h/mL | 13500 ng·h/mL | 22.4 L/kg | 45 % |
Antimalarial agent 62 (60 mg/kg administered 4 times or 160 mg/kg administered as a single dose; daily; p.o.) cures 100% of infected mice; it shows no in vivo toxicity at the tested doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CF1 (female, 7-8 weeks old, mean body weight ~30 g)[1]
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Dosage:4.5 mg/kg/day; 16.1 mg/kg/day; 60 mg/kg/day; 120 mg/kg; 160 mg/kg
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Administration:p.o.; daily for 4 days; single dose on Day 1
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Result:Achieved an ED50 of 4.5 mg/kg/day and an ED90 of 16.1 mg/kg/day in the 4-day suppression model.
Cured all 4 mice (100%) with four consecutive daily doses of 60 mg/kg/day, with no detectable parasitemia through Day 28.
Cured all 4 mice (100%) with a single 160 mg/kg dose through Day 28.
Cured 3 of 4 mice (75%) with a single 120 mg/kg dose through Day 28.
Showed no observable signs of toxicity (motor activity, grooming, posture, or body weight changes) in any treated mice.
Chemical Information
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Peso molecular 511.23
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Fòrmula C22H19Cl4N5O
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SMILES
O=C(C1=CC2=C(N=CN2CC3=CC=CC=C3)C(C4=CC(Cl)=C(C(Cl)=C4)Cl)=N1)NCCN.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antimalarial agent 62 Related Classifications
HY-183574 Related Classifications
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