Mefloquine
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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- Purity: 99.79%
- CAS No.: 53230-10-7
- 화학식: C17H16F6N2O
- 분자량:378.31
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Mefloquine
MoreAll Parasite Isoforms
More
Biological Activity
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Plasmodium |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BHK-21 | CC50 |
20.44 μM
Compound: 41
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Cytotoxicity against BHK21 cells after 24 to 48 hrs by CCK8 assay
Cytotoxicity against BHK21 cells after 24 to 48 hrs by CCK8 assay
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[PMID: 31549836] |
| Erythrocyte | IC50 |
0.014 μM
Compound: Mefloquine
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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
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[PMID: 36561069] |
| HEK293 | IC50 |
2.6 μM
Compound: mefloquine
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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
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[PMID: 25746816] |
| HepG2 | CC50 |
11.8 μM
Compound: Mfq
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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
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[PMID: 27667552] |
| HepG2 | EC50 |
9.8 μM
Compound: Mefloquine
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Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay
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[PMID: 29800827] |
| HepG2 | IC50 |
>2000 ng/mL
Compound: Mefloquine
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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
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[PMID: 24139941] |
| HepG2 | IC50 |
>2000 ng/mL
Compound: Mefloquine
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Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
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[PMID: 24139941] |
| HepG2 | IC50 |
11.5 μM
Compound: Mefloquine
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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
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[PMID: 36561069] |
| L6 | IC50 |
4.5 μM
Compound: MQ
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Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
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[PMID: 25195945] |
| Splenocyte | IC50 |
9.5 μM
Compound: Mfq
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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
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[PMID: 24530492] |
| U-251 | IC50 |
10 μM
Compound: 80
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Antiproliferative activity against human U251 cells by MTT assay
Antiproliferative activity against human U251 cells by MTT assay
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[PMID: 30583248] |
| Vero | CC50 |
21 μM
Compound: MQ
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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
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[PMID: 33636304] |
| Vero | CC50 |
212 μM
Compound: Mefloquine
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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
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[PMID: 28068604] |
| Vero | EC50 |
3.6 μM
Compound: Mefloquine
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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
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[PMID: 28068604] |
| Vero | EC50 |
3.95 μM
Compound: 41
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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
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[PMID: 31549836] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 53230-10-7
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Appearance Solid
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분자량 378.31
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화학식 C17H16F6N2O
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Color White to off-white
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SMILES
O[C@H]([C@]1([H])NCCCC1)C2=CC(C(F)(F)F)=NC3=C(C(F)(F)F)C=CC=C32
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Synonyms
Mefloquin
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
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Most Recent
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Antibiotics (Basel)
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
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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