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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 173531-57-2
分子式: C₂₄H₂₈ClN₃O
分子量:409.95

保管条件:

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

Naphthoquine 構造式

CAS 番号: 173531-57-2

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

Plasmodium

Parasite アイソフォーム固有の製品をすべて表示 :

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

体外実験

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

体内実験

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

化学情報

CAS 番号 173531-57-2
分子量 409.95
分子式 C₂₄H₂₈ClN₃O
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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