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Art. -Nr.: HY-17036A

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Naphthoquine

Naphthoquine is an orally active antimalarial and antiviral agent. Naphthoquine exhibits ex vivo activity against multidrug-resistant Plasmodium falciparum and Plasmodium vivax, preferentially targeting ring-stage rather than trophozoite-stage parasites. Naphthoquine inhibits coronavirus (SARS-CoV-2, HCoV-OC43, HCoV-229E) replication by affecting viral entry and post-entry replication. Naphthoquine is used for research on malaria and Covid-19.

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CAS. Nr.: 173531-57-2
Formel: C₂₄H₂₈ClN₃O
Molecular Weight:409.95

Speicherung:

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

Naphthoquine Chemical Structure

CAS. Nr.: 173531-57-2

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Plasmodium

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	CC₅₀	11.50 μM	Cytotoxicity against human Huh7 cells assessed as reduction in cell viability incubated for 2 days by CPE assay. Cytotoxicity against human Huh7 cells assessed as reduction in cell viability incubated for 2 days by CPE assay.	35163977
Huh-7	IC50	2.05 μM	Inhibition of HCoV-229E-induced cytopathic effect in human Huh7 cells infected with 100 TCID50 of HCoV-229E incubated for 48 hrs by CPE inhibition assay. Inhibition of HCoV-229E-induced cytopathic effect in human Huh7 cells infected with 100 TCID50 of HCoV-229E incubated for 48 hrs by CPE inhibition assay.	35163977
NCI-H460	IC50	5.83 μM	Inhibition of HCoV-OC43-induced cytopathic effect in human H460 cells infected with 100 TCID50 of HCoV-OC43 incubated for 72 hrs by CPE inhibition assay. Inhibition of HCoV-OC43-induced cytopathic effect in human H460 cells infected with 100 TCID50 of HCoV-OC43 incubated for 72 hrs by CPE inhibition assay.	35163977
Vero	CC₅₀	13.50 μM	Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability incubated for 3 days at 37 °C by MTS cell proliferation assay. Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability incubated for 3 days at 37 °C by MTS cell proliferation assay.	35163977
Vero	IC50	2.01 μM	Inhibition of SARS-CoV-2 replication in african green monkey Vero cells pretreated for 12 hrs then infected with 100 TCID50 of SARS-CoV-2 and cultured for 48 hrs post-infection, measured as reduction in viral RNA copies in supernatant by qRT-PCR. Inhibition of SARS-CoV-2 replication in african green monkey Vero cells pretreated for 12 hrs then infected with 100 TCID50 of SARS-CoV-2 and cultured for 48 hrs post-infection, measured as reduction in viral RNA copies in supernatant by qRT-PCR.	35163977

In Vitro

Parasitic InfectionViral InfectionOthers

Parasitic Infection

Naphthoquine (2-fold dilution at concentrations up to 481 nM; 35-56 h) exhibits potent ex vivo activity against field isolates of Plasmodium falciparum (median IC₅₀, 8.0 nM) and Plasmodium vivax (median IC₅₀, 7.8 nM)^[2].
Naphthoquine (2-fold serial dilution, maximum concentration of 481 nM; 24 h) exhibits stage-specific activity in Plasmodium falciparum (median IC₅₀ of 5.1 nM for rings versus median IC₅₀ of 26.5 nM for trophozoites), as well as in Plasmodium vivax (median IC₅₀ of 6.5 nM for rings versus median IC₅₀ of 341.6 nM for trophozoites)^[2].

Viral Infection

Naphthoquine (1.02-9.16 μM; 48 h) inhibits HCoV-229E replication in Huh7 cells with an IC₅₀ of 2.05 μM^[3].
Naphthoquine (1.02-9.16 μM; 72 h) inhibits HCoV-OC43 replication in H460 cells with an IC₅₀ of 5.83 μM^[3].
Naphthoquine (12 h (pretreatment); 48 h (post-infection)) inhibits SARS-CoV-2 replication in Vero cells with an IC₅₀ of 2.01 μM^[3].

Others

Naphthoquine (0.1-1.0 μg/mL; 1 h) exhibits a high plasma protein binding rate (> 80%), which is independent of sex, species, and reagent concentration in mice, rats, and humans^[1].
Naphthoquine (10 μM; 60 min) shows no sex-related differences in metabolic clearance rate in mouse and rat liver microsomes^[1].

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

Real Time qPCR^[3]

Cell Line:

Vero cells infected with SARS-CoV-2
Concentration:

Different doses
Incubation Time:

12 h (pretreatment); 48 h (post-infection)
Result:

Inhibited SARS-CoV-2 replication with an IC₅₀ of 2.01 μM.
Achieved a CC₅₀ of 13.50 μM.
Achieved a selection index of 6.72.

Parmacokinetics

Species	Dose	Route	AUC_0-t	AUC_0-∞	C_max	T_max	T_1/2	MRT	CL/F	V_z
Rat^[1]	40 mg/kg (Male) mg/kg	p.o.	36.12 μg·h/mL	37.44 μg·h/mL	504.1 ng/mL	5.4 h	192.1 h	162.6 h	1.22 L/h/kg	316.7 L/kg
Rat^[1]	40 mg/kg (Female) mg/kg	p.o.	32.82 μg·h/mL	32.70 μg·h/mL	438.1 ng/mL	3.1 h	143.9 h	173.1 h	1.27 L/h/kg	285.4 L/kg

In Vivo

Parasitic Infection

Naphthoquine (4.0 mg/kg; p.o.; single dose; 24 h post-infection) exhibits potent antiplasmodial activity in mice, with ED₉₀ values against P. yoelii of 1.10 mg/kg in males and 1.67 mg/kg in females, demonstrating comparable efficacy between the sexes^[1].

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

Animal Model:

ICR mice (male and female, 20-25 g)^[1]
Dosage:

0.71-1.67 mg/kg (ED50/ED90); 4.0 mg/kg (single dose efficacy)
Administration:

p.o.; single dose; 24 h post-infection
Result:

Achieved an ED₅₀ of 0.71 mg/kg and an ED₉₀ of 1.10 mg/kg in male mice.
Achieved an ED₅₀ of 0.94 mg/kg and an ED₉₀ of 1.67 mg/kg in female mice.
Reduced parasitaemia to less than 1.0% on day 4 post-dosing and resulted in 7 out of 9 mice surviving for at least 28 days without parasitaemia at 4.0 mg/kg.
Showed no toxicity at a dose as high as tenfold the ED50 based on weight and locomotor activity.

Related Protocols :

Research Protocol for Infectious Diseases

Chemical Information

CAS. Nr. 173531-57-2
Molecular Weight 409.95
Formel C₂₄H₂₈ClN₃O
SMILES

ClC1=CC2=NC=CC(NC3=C(CCCC4)C4=C(O)C(CNC(C)(C)C)=C3)=C2C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Xie Y, et al. The gender-related variability in the pharmacokinetics and antiplasmodial activity of naphthoquine in rodents. Malaria journal. 2020 Feb 13;19(1):71.

[2]. Wirjanata G, et al. Potent Ex Vivo Activity of Naphthoquine and Methylene Blue against Drug-Resistant Clinical Isolates of Plasmodium falciparum and Plasmodium vivax. Antimicrobial agents and chemotherapy. 2015 Oct;59(10):6117-24.

[3]. Song Y, et al. Naphthoquine: A Potent Broad-Spectrum Anti-Coronavirus Drug In Vitro. Molecules (Basel, Switzerland). 2022 Jan 21;27(3):712.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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