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Cat. No.: HY-187925

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Antimalarial agent 66

Antimalarial agent 66 is an orally effective Na⁺ATPase (PfATP-4) inhibitor and antimalarial agent with an EC₅₀ of 19 nM against the P. falciparum 3D7 strain. Antimalarial agent 66 kills malaria parasites by inhibiting PfATP-4, leading to elevated intracellular sodium ion concentration. Antimalarial agent 66 can be used for malaria research.

For research use only. We do not sell to patients.

CAS No.: 2724247-62-3
Formula: C₂₇H₂₀F₄N₄O₃
Molecular Weight:524.48

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Antimalarial agent 66 Chemical Structure

CAS No.: 2724247-62-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All Parasite Isoforms :

In Vitro

Parasitic InfectionOthers

Parasitic Infection

Antimalarial agent 66 (compound 1a) potently inhibits the growth of asexual erythrocytic-stage P. falciparum 3D7 strain (EC₅₀ = 19 nM)^[1].
Antimalarial agent 66 (1 μM; monitored for 30 min) inhibits Na⁺/H⁺-ATPase in the P. falciparum Dd2 strain (manifested as an increase in intracellular Na⁺ concentration)^[1].
Antimalarial agent 66 (up to 10 μM; 48 h) blocks malaria transmission in the P. falciparum NF54-HGL transgenic reporter strain (stage V gametocytes) (IC₅₀ = 323 nM)^[1].

Others

Antimalarial agent 66 (up to 50 μM; 48 h) exhibits low cytotoxicity in the HepG2 human cell line^[1].

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

Parmacokinetics

Species	Dose	Route	CL	T_1/2	F
Mice^[1]	10 mg/kg	p.o.	0.13 L/h/kg	17 h	79 %
Rat^[1]	3 mg/kg	p.o.	0.06 L/h/kg	26 h	107 %

In Vivo

Parasitic Infection

Antimalarial agent 66 (compound 1a) (1 mg/kg; p.o.; twice daily; 4 days) exhibits significant antimalarial efficacy in an NSG SCID mouse model engrafted with human erythrocytes and infected with P. falciparum Pf3D70087/N9^[1].

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

Animal Model:

NSG SCID mice (female) were infected with Plasmodium falciparum (Pf3D70087/N9) 72 hours before the start of drug treatment^[1]
Dosage:

1 mg/kg
Administration:

p.o.; twice daily; 1, 2, 3, 4 days
Result:

Dramatically reduced parasitemia in peripheral blood.

Chemical Information

CAS No. 2724247-62-3
Molecular Weight 524.48
Formula C₂₇H₂₀F₄N₄O₃
SMILES

C(NC1=CC(C#N)=C(F)C=C1)(=O)[C@@H]2[C@H](N(CC(F)(F)F)C(=O)C=3C2=CC=CC3)C=4C=CC(OC5CC5)=NC4
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

Handling Instructions (2659 KB)

References

[1]. Rodney Kiplin Guy, et al. Tetrahydroisoquinoline derivatives as antimalarial agents. WO2021204952A1. WIPO. 2021-10-14.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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