1. Anti-infection
  2. Parasite
  3. 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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Antimalarial agent 52

Antimalarial agent 52 Chemical Structure

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Description

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[1].

In Vitro

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.

In Vivo

Antimalarial agent 52 (Compound 7d) (3-50 mg/kg, p.o., 4, 24, 48, 72 hours after infection for 4 doses) achieves 100% cure rate at 30 and 50 mg/kg in the P. berghei mouse model[1].

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

Animal Model: P. berghei infection model established in female NMRI mice[1]
Dosage: 3, 10, 30 and 50 mg/kg
Administration: Oral administration (p.o.), 4, 24, 48, 72 hours after infection for 4 doses
Result: Showed significant dose-dependent antimalarial activity.
Molecular Weight

559.75

Formula

C24H17BrClF5N2O

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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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 52 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.

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Product Name:
Antimalarial agent 52
Cat. No.:
HY-178147
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