2. Anti-infection Metabolic Enzyme/Protease
  3. Parasite Aminopeptidase
  4. 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.

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Antimalarial agent 55

Antimalarial agent 55 Chemical Structure

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Antimalarial agent 55 Related Antibodies

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Description

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[1].

In Vitro

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.

Antimalarial agent 55 Related Antibodies
Parmacokinetics
Species Dose Route Clearance (CL) T1/2 Vss B/P Bioavailability Cmax Tmax
Mice[1] 1 mg/kg i.v. 36.1 mL/min/kg 0.86 h 0.447 L/kg 0.75 / / /
Mice[1] 3 mg/kg p.o. / 11 h / / 61.8 % 2.04 μM 0.25 h
Mice[1] 50 mg/kg p.o. / 7.2 h / / 63.4 % 20 μM 0.25 h
In Vivo

Antimalarial agent 55 (Compound 3k) (50 mg/kg; p.o.; at 2 h, 4 doses) achieves 100% antimalarial activity at 3 days post-infection in Plasmodium berghei-infected Swiss mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Arc:Arc(Swiss) (female, 6-weeks of age, intraperitoneal infection with 2 × 107 Plasmodium berghei ANKA-infected erythrocytes)[1]
Dosage: 50 mg/kg
Administration: p.o.; at 2 h, day 1, day 2, and day 3 postinfection
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.
Molecular Weight

315.37

Formula

C17H21N3O3
SMILES

CC(C)(C)CC(NC(C1=CC=C2C=CC=NC2=C1)C(NO)=O)=O
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 55 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 55Antimalarial agent55Antimalarial agent-55ParasiteAminopeptidasePlasmodium falciparum M17Plasmodium berghei M17Plasmodium berghei M1Plasmodium aminopeptidasePlasmodium falciparum M1human embryonic kidney cellsPlasmodium vivax M17Plasmodium vivax M1Plasmodium falciparum strainshuman cytochrome P450 isoformsInhibitorinhibitorinhibit

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