Mefloquine hydrochloride
Based on 4 publication(s) in Google Scholar
Mefloquine hydrochloride (Mefloquin hydrochloride), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine hydrochloride is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine hydrochloride can be used for malaria, systemic lupus erythematosus and cancer research.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 51773-92-3
- Formula: C17H17ClF6N2O
- Molecular Weight:414.77
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Mefloquine hydrochloride
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 |
|---|---|---|---|---|
| Huh-7 | CC50 |
>6.25 μM
Compound: GNF-Pf-5559
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
Mefloquine hydrochloride selectively inhibits prostate cancer (PCa) cell growth with an IC50 of ~10 μM. Mefloquine hydrochloride also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS generation[2].
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Mefloquine hydrochloride (10 μM)-mediated ROS simultaneously downregulated Akt phosphorylation and activated ERK, JNK and AMPK signaling in PC3 cells[2].
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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.
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Animal Model:Young 3.5-month-old and old 21-month-old female C57BL/6 mice[4]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; daily; 14 days
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Result:Reversed the lower vertebral cancellous bone volume and bone formation in old mice.
Chemical Information
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CAS No. 51773-92-3
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Appearance Solid
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Molecular Weight 414.77
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Formula C17H17ClF6N2O
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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.[H]Cl
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Synonyms
Mefloquin hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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
Solvent & Solubility
DMSO : 50 mg/mL (120.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2.86 mg/mL (6.90 mM; ultrasonic and warming and heat to 60°C)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: 2.5 mg/mL (6.03 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.03 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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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. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.4110 mL | 12.0549 mL | 24.1097 mL | 60.2744 mL |
| 5 mM | 0.4822 mL | 2.4110 mL | 4.8219 mL | 12.0549 mL | |
| DMSO | 10 mM | 0.2411 mL | 1.2055 mL | 2.4110 mL | 6.0274 mL |
| 15 mM | 0.1607 mL | 0.8037 mL | 1.6073 mL | 4.0183 mL | |
| 20 mM | 0.1205 mL | 0.6027 mL | 1.2055 mL | 3.0137 mL | |
| 25 mM | 0.0964 mL | 0.4822 mL | 0.9644 mL | 2.4110 mL | |
| 30 mM | 0.0804 mL | 0.4018 mL | 0.8037 mL | 2.0091 mL | |
| 40 mM | 0.0603 mL | 0.3014 mL | 0.6027 mL | 1.5069 mL | |
| 50 mM | 0.0482 mL | 0.2411 mL | 0.4822 mL | 1.2055 mL | |
| 60 mM | 0.0402 mL | 0.2009 mL | 0.4018 mL | 1.0046 mL | |
| 80 mM | 0.0301 mL | 0.1507 mL | 0.3014 mL | 0.7534 mL | |
| 100 mM | 0.0241 mL | 0.1205 mL | 0.2411 mL | 0.6027 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mefloquine hydrochloride Related Classifications
HY-17437A Related Classifications
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