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Referencia número: HY-181266

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Antimalarial agent 55

Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with K_i 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 K_i 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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Fòrmula: C₁₇H₂₁N₃O₃
Peso molecular:315.37

Almacenamiento:

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

Data Sheet (272 KB)

Antimalarial agent 55 Chemical Structure

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

Actividad biológica
- Descripciòn
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas Parasite :

Ver todos los productos específicos de isoformas Aminopeptidase :

CD13
LTA4H

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.

Parmacokinetics

Species	Dose	Route	Clearance (CL)	T_1/2	V_ss	B/P	Bioavailability	C_max	T_max
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.

Chemical Information

Peso molecular 315.37
Fòrmula C₁₇H₂₁N₃O₃
SMILES

CC(C)(C)CC(NC(C1=CC=C2C=CC=NC2=C1)C(NO)=O)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Mansouri M, et al. Novel Scaffold Unlocks Potent Cross-Peptidase and Cross-Species Inhibitors as Promising Antimalarial Agents. J Med Chem. 2026;69(2):1358-1386. [Content Brief]

Calculators

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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Antimalarial agent 55

Ver todos los productos específicos de isoformas Parasite

Ver todos los productos específicos de isoformas Aminopeptidase

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

Antimalarial agent 55 Related Classifications

HY-181266 Related Classifications