| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 10g |
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Purity: ≥98%
Mefloquine HCl (Mefloquin) is a blood schizonticide which inhibits hemozoin formation, and is used as a phospholipid-interacting antimalarial drug. Mefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. Mefloquine can induces oxidative stress in vitro. Evidence indicates that reactive oxygen species (ROS) may be used as a therapeutic modality to kill cancer cell. Mefloquine inhibited KvLQT1/minK channel currents with an IC50 value of approximately 1 μM. Mefloquine slowed the activation rate of KvLQT1/minK and more block was evident at lower membrane potentials compared with higher ones.
| Targets |
Plasmodium
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| ln Vitro |
Mefloquine is a quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine. Mefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. MQ can induces oxidative stress in vitro. Evidence indicates that reactive oxygen species (ROS) may be used as a therapeutic modality to kill cancer cells.
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| ln Vivo |
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| Cell Assay |
Mefloquine inhibitedKvLQT1/minK channel currents with an IC50 value of approximately 1 microM. Mefloquine slowed the activation rate of KvLQT1/minK and more block was evident at lower membrane potentials compared with higher ones. HERG channel currents were about 6-fold less sensitive to block by mefloquine (IC50 = 5.6 microM). Block of HERG displayed a positive voltage dependence with maximal inhibition obtained at more depolarized potentials. MQ has a highly selective cytotoxicity that inhibits PCa cell growth. MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells.
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| References |
| Molecular Formula |
C17H17CLF6N2O
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|---|---|
| Molecular Weight |
414.77
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| Elemental Analysis |
C, 49.23; H, 4.13; Cl, 8.55; F, 27.48; N, 6.75; O, 3.86
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| CAS # |
51773-92-3
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| Related CAS # |
Mefloquine;53230-10-7
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| Appearance |
White to light yellow crystalline powder.
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| SMILES |
C1CCN[C@H](C1)[C@H](C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O.Cl
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| InChi Key |
WESWYMRNZNDGBX-YLCXCWDSSA-N
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| InChi Code |
InChI=1S/C17H16F6N2O.ClH/c18-16(19,20)11-5-3-4-9-10(15(26)12-6-1-2-7-24-12)8-13(17(21,22)23)25-14(9)11;/h3-5,8,12,15,24,26H,1-2,6-7H2;1H/t12-,15+;/m1./s1
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| Chemical Name |
(S)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2R)-piperidin-2-yl]methanol;hydrochloride
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| Synonyms |
Mefloquine Hydrochloride; Mephaquin; Mefloquine HCL; Loriam; Mefloquine (hydrochloride); WR-177,602; WR142,490; WR177,602; Ro215998001; Roche; Brand of Mefloquine Hydrochloride;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol :~83 mg/mL
H2O :~2.86 mg/mL (~6.90 mM) DMSO : ~50 mg/mL ( ~120.54 mM ) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.03 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (6.03 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (6.03 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4110 mL | 12.0549 mL | 24.1097 mL | |
| 5 mM | 0.4822 mL | 2.4110 mL | 4.8219 mL | |
| 10 mM | 0.2411 mL | 1.2055 mL | 2.4110 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00746941 | Terminated | Drug: mefloquine | Progressive Multifocal Leukoencephalopathy |
Biogen | January 2009 | Phase 1 Phase 2 |
| NCT01430351 | Active,not recruiting | Drug: Mefloquine Drug: Temozolomide |
Glioblastoma Gliosarcoma |
M.D. Anderson Cancer Center |
September 14, 2011 | Phase 1 |
| NCT03923725 | Recruiting | Drug: Artesunate-mefloquine +placebo (AS-MQ+PBO) |
Plasmodium Falciparum Malaria (Uncomplicated) |
University of Oxford | September 1, 2020 | Phase 3 |
| NCT05690841 | Not yet recruiting | Drug: Focal Mass Drug Administration (fMDA) |
Malaria, Vivax Malaria |
University of California, San Francisco |
June 1, 2024 | Phase 3 |
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