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 No.: 173531-57-2
- Formule: C24H28ClN3O
- Masse moléculaire:409.95
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
Plasmodium |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
11.50 μM
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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.
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35163977 |
| Huh-7 | IC50 |
2.05 μM
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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.
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35163977 |
| NCI-H460 | IC50 |
5.83 μM
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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.
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35163977 |
| Vero | CC50 |
13.50 μM
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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.
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35163977 |
| Vero | IC50 |
2.01 μM
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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.
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35163977 |
In Vitro
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].
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].
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.
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Cell Line:Vero cells infected with SARS-CoV-2
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Concentration:Different doses
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Incubation Time:12 h (pretreatment); 48 h (post-infection)
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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
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male and female, 20-25 g)[1]
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Dosage:0.71-1.67 mg/kg (ED50/ED90); 4.0 mg/kg (single dose efficacy)
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Administration:p.o.; single dose; 24 h post-infection
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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.
Chemical Information
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CAS No. 173531-57-2
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Masse moléculaire 409.95
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Formule C24H28ClN3O
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SMILES
ClC1=CC2=NC=CC(NC3=C(CCCC4)C4=C(O)C(CNC(C)(C)C)=C3)=C2C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Naphthoquine Related Classifications
HY-17036A Related Classifications
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Keywords
- Naphthoquine
- 173531-57-2
- Parasite
- SARS-CoV
- 4-aminoquinoline antimalarial agent
- coronavirus replication
- CYP2D6-dependent hydroxylation
- blood-stage Plasmodium
- N-oxidation metabolism
- Plasmodium vivax
- Acinetobacter baumannii
- angiotensin-converting enzyme 2
- haemozoin formation
- Plasmodium falciparum
- Inhibitor
- inhibitor
- inhibit