Art. -Nr.: HY-17437

Mefloquine

(Synonyms: Mefloquin)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K⁺ channel (KvQT1/minK) antagonist with an IC₅₀ of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.

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Reinheit: 99.79%
CAS. Nr.: 53230-10-7
Formel: C₁₇H₁₆F₆N₂O
Molecular Weight:378.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Mefloquine Chemical Structure

CAS. Nr.: 53230-10-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Plasmodium

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BHK-21	CC₅₀	20.44 μM Compound: 41	Cytotoxicity against BHK21 cells after 24 to 48 hrs by CCK8 assay Cytotoxicity against BHK21 cells after 24 to 48 hrs by CCK8 assay	[PMID: 31549836]
Erythrocyte	IC₅₀	0.014 μM Compound: Mefloquine	Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay	[PMID: 36561069]
HEK293	IC₅₀	2.6 μM Compound: mefloquine	Inhibition of human ERG expressed in HEK293 cells assessed as reduction in tail current at membrane potential of +20 mV Inhibition of human ERG expressed in HEK293 cells assessed as reduction in tail current at membrane potential of +20 mV	[PMID: 25746816]
HepG2	CC₅₀	11.8 μM Compound: Mfq	Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by alamar blue assay Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by alamar blue assay	[PMID: 27667552]
HepG2	EC₅₀	9.8 μM Compound: Mefloquine	Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29800827]
HepG2	IC₅₀	>2000 ng/mL Compound: Mefloquine	Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay	[PMID: 24139941]
HepG2	IC₅₀	>2000 ng/mL Compound: Mefloquine	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 24139941]
HepG2	IC₅₀	11.5 μM Compound: Mefloquine	Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence assay Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence assay	[PMID: 36561069]
L6	IC₅₀	4.5 μM Compound: MQ	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 25195945]
Splenocyte	IC₅₀	9.5 μM Compound: Mfq	Cytotoxicity against BALB/c mouse splenocytes assessed as [3H]-thymidine incorporation after 24 hrs by beta-radiation counting analysis relative to control Cytotoxicity against BALB/c mouse splenocytes assessed as [3H]-thymidine incorporation after 24 hrs by beta-radiation counting analysis relative to control	[PMID: 24530492]
U-251	IC₅₀	10 μM Compound: 80	Antiproliferative activity against human U251 cells by MTT assay Antiproliferative activity against human U251 cells by MTT assay	[PMID: 30583248]
Vero	CC₅₀	21 μM Compound: MQ	Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell proliferation Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell proliferation	[PMID: 33636304]
Vero	CC₅₀	212 μM Compound: Mefloquine	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by XTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by XTT assay	[PMID: 28068604]
Vero	EC₅₀	3.6 μM Compound: Mefloquine	Antiviral activity against Zika virus infected in African green monkey Vero cells assessed as inhibition of viral RNA replication after 24 hrs by RT-PCR method Antiviral activity against Zika virus infected in African green monkey Vero cells assessed as inhibition of viral RNA replication after 24 hrs by RT-PCR method	[PMID: 28068604]
Vero	EC₅₀	3.95 μM Compound: 41	Antiviral activity against Zika virus MR766 infected in African green monkey Vero cells by plaque assay Antiviral activity against Zika virus MR766 infected in African green monkey Vero cells by plaque assay	[PMID: 31549836]

In Vitro

Mefloquine selectively inhibits prostate cancer (PCa) cell growth with an IC₅₀ of ~10 μM. Mefloquine also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS generation^[2].
Mefloquine (10 μM)-mediated ROS simultaneously downregulated Akt phosphorylation and activated ERK, JNK and AMPK signaling in PC3 cells^[2].
Mefloquine shows higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC₅₀ of 1.28 μM, IC₉₀ of 2.31 μM, and IC₉₉ of 4.39 μM in VeroE6/TMPRSS2 cells. Mefloquine inhibits viral entry after viral attachment to the target cell^[3].

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

In Vivo

Mefloquine (5 mg/kg; i.p.; daily; 14 days) reverses the lower vertebral cancellous bone volume and bone formation; and has modest effects on cortical bone volume, thickness, and moment of inertia in old mice^[4].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 53230-10-7
Appearance Solid
Molecular Weight 378.31
Formel C₁₇H₁₆F₆N₂O
Color White to off-white
SMILES

O[C@H]([C@]1([H])NCCCC1)C2=CC(C(F)(F)F)=NC3=C(C(F)(F)F)C=CC=C32
Synonyms

Mefloquin
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Journal Impact Factor

Antibiotics (Basel)

Evaluation of the Efficacy of Anthelmintic Drugs Against Trichinella spiralis Larvae. [Abstract]

2026 Feb 16;15(2):215. PMID: 41750512
ACS Omega

Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. [Abstract]

2024 Feb 28;9(10):11870-11882. PMID: 38496939
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
Front Oncol

Mefloquine Inhibits Esophageal Squamous Cell Carcinoma Tumor Growth by Inducing Mitochondrial Autophagy. [Abstract]

2020 Jul 28;10:1217. PMID: 32850358

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 200 mg/mL (528.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6433 mL

13.2167 mL

26.4333 mL

5 mM

0.5287 mL

2.6433 mL

5.2867 mL

10 mM

0.2643 mL

1.3217 mL

2.6433 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (13.22 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (13.22 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

Verweise

[1]. Kang J, et al. Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK andHERG. J Pharmacol Exp Ther. 2001 Oct;299(1):290-6. [Content Brief]

[2]. Yan KH, et al. Mefloquine exerts anticancer activity in prostate cancer cells via ROS-mediated modulation of Akt, ERK, JNK and AMPK signaling. Oncol Lett. 2013 May;5(5):1541-1545. [Content Brief]

[3]. Kaho Shionoya, et al. Mefloquine, a Potent Anti-severe Acute Respiratory Syndrome-Related Coronavirus 2 (SARS-CoV-2) Drug as an Entry Inhibitor in vitro. Front Microbiol. 2021 Apr 30;12:651403. [Content Brief]

[4]. Rafael Pacheco-Costa, et al. Reversal of loss of bone mass in old mice treated with mefloquine. Bone. 2018 Sep;114:22-31. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6433 mL	13.2167 mL	26.4333 mL	66.0834 mL
	5 mM	0.5287 mL	2.6433 mL	5.2867 mL	13.2167 mL
	10 mM	0.2643 mL	1.3217 mL	2.6433 mL	6.6083 mL
	15 mM	0.1762 mL	0.8811 mL	1.7622 mL	4.4056 mL
	20 mM	0.1322 mL	0.6608 mL	1.3217 mL	3.3042 mL
	25 mM	0.1057 mL	0.5287 mL	1.0573 mL	2.6433 mL
	30 mM	0.0881 mL	0.4406 mL	0.8811 mL	2.2028 mL
	40 mM	0.0661 mL	0.3304 mL	0.6608 mL	1.6521 mL
	50 mM	0.0529 mL	0.2643 mL	0.5287 mL	1.3217 mL
	60 mM	0.0441 mL	0.2203 mL	0.4406 mL	1.1014 mL
	80 mM	0.0330 mL	0.1652 mL	0.3304 mL	0.8260 mL
	100 mM	0.0264 mL	0.1322 mL	0.2643 mL	0.6608 mL

Mefloquine

4 Cited Publications

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Mefloquine

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Publications Citing Use of MedChemExpress (MCE) Mefloquine

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mefloquine Related Classifications

Art. -Nr.: HY-17437