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Cat. No.: HY-187926

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Antimalarial agent 67

Antimalarial agent 67 is an orally active inositol acyltransferase Gwt1p inhibitor and antimalarial agent, with IC₅₀ values of 0.030 μM and 0.041 μM against P. falciparum 3D7 and K1 strains, respectively. Antimalarial agent 67 blocks inositol ring acylation by inhibiting the key enzyme Gwt1p in the GPI biosynthesis pathway of Plasmodium, thereby inhibiting parasite growth and maturation. Antimalarial agent 67 can be used for research on malaria.

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CAS No.: 2675491-09-3
Formule: C₂₁H₁₉F₆N₇O₂
Masse moléculaire:515.42

Stockage:

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

Antimalarial agent 67 Chemical Structure

CAS No.: 2675491-09-3

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

Activité biologique
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- In Vitro
- In Vivo
Chemical Information
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Description

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In Vitro

Parasitic Infection

Antimalarial agent 67 (compound VII) (0.001-1 μg/mL; 72 h) exhibits antimalarial activity against the erythrocytic stages of P. falciparum 3D7 and K1 strains in vitro, with IC₅₀ values of 0.030 μM and 0.041 μM, respectively^[1].

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

In Vivo

Parasitic Infection

Antimalarial agent 67 (Compound VII) (10 mL/kg; p.o.; once daily; for 3 consecutive days) exhibits antimalarial activity in a humanized immunodeficient NSG 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 (NOD-scid IL-2RYnull) mice (female) were infected with P. falciparum (Pf3D70087/N9)^[1]
Dosage:

10 mL/kg
Administration:

p.o.; once daily; for 3 consecutive days
Result:

Demonstrated in vivo antimalarial efficacy, being able to significantly reduce parasitemia in peripheral blood. The daily dose that reduced parasitemia by 90% compared to untreated control animals at day seven post-infection (ED90) was 6.2 mg/kg/day.

Chemical Information

CAS No. 2675491-09-3
Masse moléculaire 515.42
Formule C₂₁H₁₉F₆N₇O₂
SMILES

O=C(NCC1=CC=C(OCC(F)(F)F)C=C1)C=2C=C(C(=NC2N)N)N3N=C(N=C3)C4(CC4)C(F)(F)F
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Takaaki Horii, et al. Novel antimalarial agent containing heterocyclic compound. WO2021149692A1. WIPO. 2021-07-29.

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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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Activité biologique
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- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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Antimalarial agent 67

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