Antimalarial agent 55
Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodium vivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria research.
For research use only. We do not sell to patients.
- Formula: C17H21N3O3
- Molecular Weight:315.37
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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
Antimalarial agent 55 (Compound 3k) (72 h) exhibits in vitro killing activity against the Plasmodium falciparum strain Pf3D7, with an EC50 of 31 nM; it also shows potent activity against clinically isolated Plasmodium falciparum strains with different drug resistance mechanisms.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Arc:Arc(Swiss) (female, 6-weeks of age, intraperitoneal infection with 2 × 107 Plasmodium berghei ANKA-infected erythrocytes)[1]
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Dosage:50 mg/kg
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Administration:p.o.; at 2 h, day 1, day 2, and day 3 postinfection
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Result:Achieved 100% antimalarial activity at 3 days post-infection.\nAchieved 83% antimalarial activity at 4 days post-infection.\nAchieved 63% antimalarial activity at 6 days post-infection.
Chemical Information
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Molecular Weight 315.37
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Formula C17H21N3O3
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SMILES
CC(C)(C)CC(NC(C1=CC=C2C=CC=NC2=C1)C(NO)=O)=O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Antimalarial agent 55
- Antimalarial agent55
- Antimalarial agent-55
- Parasite
- Aminopeptidase
- Plasmodium falciparum M17
- Plasmodium berghei M17
- Plasmodium berghei M1
- Plasmodium aminopeptidase
- Plasmodium falciparum M1
- human embryonic kidney cells
- Plasmodium vivax M17
- Plasmodium vivax M1
- Plasmodium falciparum strains
- human cytochrome P450 isoforms
- Inhibitor
- inhibitor
- inhibit