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Chemical Structure| 51773-92-3 Chemical Structure| 51773-92-3

Structure of Mefloquine HCI
CAS No.: 51773-92-3

Chemical Structure| 51773-92-3

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CAS No.: 51773-92-3

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Mefloquine HCl is a quinolinemethanol derivative with antimalarial properties.

Synonyms: Mefloquin hydrochloride; Ro 21-5998/001; NSC 157387

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Product Details of Mefloquine HCI

CAS No. :51773-92-3
Formula : C17H17ClF6N2O
M.W : 414.77
SMILES Code : O[C@@H](C1=CC(C(F)(F)F)=NC2=C(C(F)(F)F)C=CC=C12)[C@@H]3NCCCC3.[H]Cl
Synonyms :
Mefloquin hydrochloride; Ro 21-5998/001; NSC 157387
MDL No. :MFCD00797519

Safety of Mefloquine HCI

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Cx36-transfected N2A neuroblastoma cells 300 nM To evaluate the blocking effect of mefloquine on Cx36 channels, results showed IC50≈300 nM. PMC514481
Cx43-transfected N2A neuroblastoma cells 30 μM To evaluate the blocking effect of mefloquine on Cx43 channels, results showed 30 μM concentration could completely block. PMC514481
Cx50-transfected N2A neuroblastoma cells 1.1 μM To evaluate the blocking effect of mefloquine on Cx50 channels, results showed IC50≈1.1 μM. PMC514481
IO neurons 50 μM Block gap junctions, reducing electrical coupling between IO neurons PMC1925036
Cortical interneurons 25–50 μM Block gap junctions, reducing electrical coupling between cortical interneurons PMC1925036

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Hippocampal and neocortical slices Perfusion 25 μM 70-100 minutes To evaluate the blocking effect of mefloquine on electrical coupling between interneurons in neocortical slices, results showed 25 μM concentration significantly blocked coupling. PMC514481
Mice Thoracodorsal resistance arteries (TDA) 10 μmol/L Single dose To investigate the effect of mefloquine on PE-induced vasoconstriction, results showed that mefloquine significantly reduced PE-induced vasoconstriction. PMC3135971
Mice Malaria model Subcutaneous injection 40 mg/kg 4 consecutive days Evaluate mefloquine resistance in malaria parasites PMC10899652
NOD/SCID mice Human RBC engrafted model Oral 40 mg/kg Once daily for 3 days To evaluate hemolytic toxicity of mefloquine in G6PD-deficient human RBC engrafted mice, results showed no significant hemolysis PMC3808620

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01976325 Malaria Not Applicable Unknown November 2015 Canada, Ontario ... More >> National Capital Region Occupational Health Clinic Recruiting Ottawa, Ontario, Canada, K1A 0K9 Contact: Louise J Levesque, RN, BScN ?? 613-946-5533 ?? louise.j.levesque@hc-sc.gc.ca ?? Contact: Lisa Taras, MD, CCFP ?? 613-946-6583 ?? lisa.taras@hc-sc.gc.ca ?? Ottawa Hospital Research Institute Recruiting Ottawa, Ontario, Canada, K1Y 4E9 Contact: Charde A Morgan, MScPH ?? 613-737-8899 ext 72424 ?? cmorgan@ohri.ca ?? Contact: Anne E McCarthy, MD ?? 613-737-8899 ext 78184 ?? amccarthy@toh.on.ca ?? Principal Investigator: Anne E McCarthy, MD, MSc ?? ?? ?? Sub-Investigator: Charde A Morgan, MScPH ?? ?? ?? International Association for Medical Assistance to Travellers Recruiting Toronto, Ontario, Canada, M6K 3E3 Contact: Tullia Marcolongo ?? 416-652-0137 ?? tullia@iamat.org Less <<
NCT00902811 Uncomplicated Falciparum Malar... More >>ia Less << Phase 4 Unknown December 2009 Myanmar ... More >> Dabhine and Mingan Clinic Recruiting Sittwe, Rakhine, Myanmar Contact: Pyay Phyo Aung ?? ?? frank_smithuis@yahoo.com ?? Principal Investigator: Pyay Phyo Aung, MD ?? ?? ?? Myit Kyi Nar Clinic Recruiting Kachin, Myanmar Contact: Mya Nee Nyo ?? ?? frank_smithuis@yahoo.com ?? Principal Investigator: Mya Nee Nyo, MD ?? ?? ?? Myothugyi Rural Health Center, Bu Thee Daung Recruiting Maungdaw, Myanmar Contact: Arkar Linn Naing ?? ?? frank_smithuis@yahoo.com ?? Principal Investigator: Arkar Linn Naing, MD ?? ?? ?? Lashio Clinic Recruiting Shan, Myanmar Contact: Naing Nyo, MD ?? ?? ?? Principal Investigator: Naing Zaw, MD Less <<
NCT01107145 Plasmodium Vivax Malaria Phase 4 Terminated(Extremely slow enro... More >>llment) Less << - Brazil ... More >> Hospital Geral Maternidade de Cruzeiro do Sul Cruzeiro do Sul, Acre, Brazil Hospital Municipal Teonila Alves Anajas, Para, Brazil Centro de Pesquisa em Patologias Tropicais Porto Velho, Rondonia, Brazil Less <<
NCT01430351 Brain Cancer Phase 1 Active, not recruiting September 2019 United States, Texas ... More >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT00746941 Progressive Multifocal Leukoen... More >>cephalopathy Less << Phase 1 Phase 2 Terminated(Primary endpoint no... More >>t achieved) Less << - United States, Illinois ... More >> Research Site Chicago, Illinois, United States United States, Maryland Research Site Baltimore, Maryland, United States United States, Massachusetts Research Site Boston, Massachusetts, United States United States, Missouri Research Site St. Louis, Missouri, United States United States, New York Research Site New York, New York, United States Brazil Research Site Sao Paulo, Brazil Germany Research Site Dusseldorf, North Rhine-Westphalia, Germany Research Site Berlin, Germany Research Site Hamburg, Germany Italy Research Site Milano, Italy Spain Research Site Barcelona, Spain Research Site Madrid, Spain Less <<
NCT00444106 - Completed - -
NCT00978172 Malaria Phase 4 Completed - Cameroon ... More >> Centre Mère et Enfant, Fondation Chantal Biya Yaounde, Cameroon, BP 1936 Less <<
NCT00746941 - Terminated(Primary endpoint no... More >>t achieved) Less << - -
NCT01082718 Malaria Pregn... More >>ancy Less << Phase 2 Phase 3 Withdrawn(Logistical difficult... More >>ies) Less << October 2010 -
NCT02453308 Malaria, Falciparum Phase 2 Phase 3 Completed - Bangladesh ... More >> College of Medicine Chittagong Ramu, Bangladesh Cambodia Pailin Pailin, Cambodia Preah Vihear Preah Vihear, Cambodia Pursat Pursat, Cambodia Ratanakiri Ratankiri, Cambodia Congo, The Democratic Republic of the Kinshasa Kinshasa, Congo, The Democratic Republic of the India Mohanpur Community health center Agartala, India Midnapore Midnapore, India Ispat General hospital Rourkela, India Lao People's Democratic Republic Sekong Sekong, Lao People's Democratic Republic Myanmar Ann Hospital Ann, Myanmar Pyay hospital Pyay, Myanmar Pyin oo Lwin hospital Pyin oo Lwin, Myanmar Thabeikkyin hospital Thabeikkyin, Myanmar Thailand Phusing hospital Phusing, Srisaket, Thailand Tha Song Yang hospital Tha Song Yang, Tak, Thailand Chumphon hospital Chumphon, Thailand Kunhan Hospital Si Sa Ket, Thailand Thanto Hospital Yala, Thailand Vietnam Binh Phuoc hospital Binh Phuoc, Vietnam Less <<
NCT00544024 - Completed - Peru ... More >> Apoyo Hospital Iquitos, Peru Less <<
NCT00444106 Malaria Falci... More >>parum Less << Phase 4 Completed - Colombia ... More >> Novartis Investigational Site Tumaco, Colombia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.05mL

2.41mL

1.21mL

24.11mL

4.82mL

2.41mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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