Mefloquine HCl (Mefloquin)

Alias: Mefloquine Hydrochloride; Mephaquin; Mefloquine HCL; Loriam; Mefloquine (hydrochloride); WR-177,602; WR142,490; WR177,602; Ro215998001; Roche; Brand of Mefloquine Hydrochloride;
Cat No.:V1908 Purity: ≥98%
Mefloquine HCl(Mefloquin) is a blood schizonticide which inhibits hemozoin formation, and is used as aphospholipid-interacting antimalarial drug.
Mefloquine HCl (Mefloquin) Chemical Structure CAS No.: 51773-92-3
Product category: Parasite
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of Mefloquine HCl (Mefloquin):

  • Mefloquine (Mefloquin)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
Plasmodium
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.
ln Vivo
Pregnant rats were treated orally with AS (15 and 40 mg/kg body weight (bwt)/day), MQ (30 and 80 mg/kg bwt/day) and AS/MQ (15/30 and 40/80 mg/kg bwt/day) on days 9-11 post coitum (pc). The dams were euthanized on day 12 pc and gestational and embryos histological parameters were evaluated.
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.
Animal Protocol
30 and 80 mg/kg; oral gavage
Rats
References

[1]. 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.

[2]. 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.

[3]. 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.

[4]. Reversal of loss of bone mass in old mice treated with mefloquine. Bone. 2018 Sep;114:22-31.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H17CLF6N2O
Molecular Weight
414.77
Elemental Analysis
C, 49.23; H, 4.13; Cl, 8.55; F, 27.48; N, 6.75; O, 3.86
CAS #
51773-92-3
Appearance
White to light yellow crystalline powder.
SMILES
C1CCN[C@H](C1)[C@H](C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O.Cl
InChi Key
WESWYMRNZNDGBX-YLCXCWDSSA-N
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
Chemical Name
(S)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2R)-piperidin-2-yl]methanol;hydrochloride
Synonyms
Mefloquine Hydrochloride; Mephaquin; Mefloquine HCL; Loriam; Mefloquine (hydrochloride); WR-177,602; WR142,490; WR177,602; Ro215998001; Roche; Brand of Mefloquine Hydrochloride;
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
Ethanol :~83 mg/mL
H2O :~2.86 mg/mL (~6.90 mM)
DMSO : ~50 mg/mL ( ~120.54 mM )
Solubility (In Vivo)
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (6.03 mM) (Please use freshly prepared in vivo formulations for optimal results.)
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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

Biological Data
  • Inhibition of the proliferation of prostate cancer (PCa) cells by mefloquine (MQ) in vitro. [2]. Oncol Lett. 2013 May;5(5):1541-1545.
  • Antitumor effect of mefloquine (MQ) in DU145 and PC3 cells was assayed by colony formation assay.[2]. Oncol Lett. 2013 May;5(5):1541-1545.
  • Effect of mefloquine (MQ)-induced alteration of mitochondrial membrane potential (MMP) and reactive oxygen species (ROS) generation in PCa cells. [2]. Oncol Lett. 2013 May;5(5):1541-1545.
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