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  4. 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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Antimalarial agent 62

Antimalarial agent 62 Chemical Structure

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Antimalarial agent 62 Related Antibodies

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Description

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[1].

IC50 & Target

Plasmodium

 

Parmacokinetics
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 %
In Vivo

Antimalarial agent 62 (10b) (4.5-160 mg/kg; p.o.; for 4 consecutive days) exhibits an ED50 of 4.5 mg/kg/d and an ED90 of 16.1 mg/kg/d in mice, and reduces P. yoelii parasitemia by 50% at the ED50 dose[1].
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.

Animal Model: CF1 (female, 7-8 weeks old, mean body weight ~30 g)[1]
Dosage: 4.5 mg/kg/day; 16.1 mg/kg/day; 60 mg/kg/day; 120 mg/kg; 160 mg/kg
Administration: p.o.; daily for 4 days; single dose on Day 1
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.
Molecular Weight

511.23

Formula

C22H19Cl4N5O
SMILES

O=C(C1=CC2=C(N=CN2CC3=CC=CC=C3)C(C4=CC(Cl)=C(C(Cl)=C4)Cl)=N1)NCCN.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Antimalarial agent 62 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Antimalarial agent 62Antimalarial agent62Antimalarial agent-62ParasitemicePlasmodium yoeliimalariaAReBaR resistome screendihydroartemisinin-induced dormant Plasmodium ringsPlasmodium ringsInhibitorinhibitorinhibit

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