[CAS NO. 51773-92-3] Mefloquinehydrochloride

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PRODUCTS SPECIFICATIONS [51773-92-3]

Catalog

HY-17437A

Brand

MCE

CAS

51773-92-3

DESCRIPTION [51773-92-3]

Overview

MDL	MFCD00797519
Molecular Weight	414.77
Molecular Formula	C17H17ClF6N2O
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

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

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 IC ₅₀ of ~1 μM. Mefloquine hydrochloride can be used for malaria, systemic lupus erythematosus and cancer research ^[1] ^[2] ^[3] .

IC50 & Target

Plasmodium

In Vitro

Mefloquine hydrochloride selectively inhibits prostate cancer (PCa) cell growth with an IC ₅₀ of ~10 μM. Mefloquine hydrochloride also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS generation ^[2] .
Mefloquine hydrochloride (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 IC ₅₀ of 1.28 μM, IC ₉₀ of 2.31 μM, and IC ₉₉ of 4.39 μM in VeroE6/TMPRSS2 cells. Mefloquine inhibits viral entry after viral attachment to the target cell ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mefloquine hydrochloride (5 mg/kg; i.p.; daily; 14 days) reverses the lower vertebral cancellous bone volume and bone formation; and has modest effects on cortical bone volume, thickness, and moment of inertia in old mice ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Young 3.5-month-old and old 21-month-old female C57BL/6 mice ^[4]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; daily; 14 days
Result:	Reversed the lower vertebral cancellous bone volume and bone formation in old mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04847661	Helwan University\|Ain Shams University\|Fayoum University\|Assiut University\|Tanta University\|National Institute of Infectious Diseases, Tokyo, Japan	Covid19	March 28, 2021	Phase 2\|Phase 3
NCT02653898	Armed Forces Research Institute of Medical Sciences, Thailand\|National Center for Parasitology, Entomology, and Malaria Control (CNM)\|Ministry of National Defense, Royal Cambodian Armed Forces Department of Health	Malaria\|Parasitic Diseases	January 2016	Phase 4
NCT01976780	Global Emerging Infections Surveillance and Response System\|United States Army Medical Unit - Kenya\|Walter Reed Army Institute of Research (WRAIR)	Malaria	June 2013	Phase 4
NCT02488980	U.S. Army Medical Research and Development Command\|SmithKline Beecham	Falciparum Parasitaemia	May 2000	Phase 2
NCT00978172	Mepha Ltd.\|Centre Mère et Enfant de la Fondation Chantal Biya	Malaria	December 2007	Phase 4
NCT00761020	U.S. Army Medical Research and Development Command\|Walter Reed Army Institute of Research (WRAIR)	Malaria	September 2008	Not Applicable
NCT01082718	Centers for Disease Control and Prevention	Malaria\|Pregnancy	March 2010	Phase 2\|Phase 3
NCT00499876	London School of Hygiene and Tropical Medicine\|Noguchi Memorial Institute for Medical Research	HIV Infections\|Malaria	October 2007	Not Applicable
NCT02524444	ORIYOMI OMOTOYOSI AKINYOTU\|University of Ibadan	Malaria in Pregnant HIV &addition; Patients	September 2015	Phase 1
NCT00322907	Center for Primary Care and Public Health (Unisante), University of Lausanne, Switzerland\|Papua New Guinea Institute of Medical Research\|Swiss Tropical & Public Health Institute	Clinical Malaria	April 2000	Phase 2
NCT04347031	Burnasyan Federal Medical Biophysical Center	Pneumonia, Viral\|Respiratory Failure	April 8, 2020	Phase 2\|Phase 3
NCT01132248	Albert Schweitzer Hospital	Urinary Schistosomiasis	May 2010	Phase 2
NCT00746941	Biogen\|Elan Pharmaceuticals	Progressive Multifocal Leukoencephalopathy	January 2009	Phase 1\|Phase 2
NCT00403260	Medicines for Malaria Venture\|Shin Poong Pharmaceuticals	Falciparum Malaria	January 2007	Phase 3
NCT01939886	London School of Hygiene and Tropical Medicine\|Kilimanjaro Christian Medical Centre, Tanzania\|Radboud University Medical Center\|European Union	Malaria	April 2013	Phase 3
NCT02974348	University of Bamenda\|Ministry of Science and Technology of the People´s Republic of China\|National Institute for Parasitic Disease, Chinese Center for Disease Control and Prevention	Drug Resistant Malaria Due to Plasmodium Falciparum	January 2013	Phase 3
NCT00373048	Institute of Tropical Medicine, Belgium	HIV Infections	October 2005	Not Applicable
NCT01422954	Radboud University Medical Center\|ZonMw: The Netherlands Organisation for Health Research and Development	Malaria\|Plasmodium Falciparum	January 2012	Not Applicable
NCT00811421	Hospital Clinic of Barcelona\|Barcelona Centre for International Health Research\|Institute of Tropical Medicine, University of Tuebingen\|Institut de Recherche pour le Developpement\|Université d´Abomey-Calavi\|Albert Schweitzer Hospital\|Kenya Medical Research Institute\|Ifakara Health Institute\|Centro de Investigacao em Saude de Manhica\|Vienna School of Clinical Research (VSCR), Austria.\|Centers for Disease Control and Prevention\|Malaria in Pregnancy Consortium	Pregnancy\|Malaria\|HIV Infections	September 2009	Not Applicable
NCT01319448	London School of Hygiene and Tropical Medicine\|Medical Research Council Unit, The Gambia\|Wellcome Trust\|University of Ilorin Teaching Hospital	Malaria\|Sickle Cell Crisis	September 2011	Phase 1\|Phase 2
NCT03726593	Armed Forces Research Institute of Medical Sciences, Thailand\|National Center for Parasitology, Entomology, and Malaria Control (CNM)\|Naval Medical Research Unit-2 (NAMRU-2)	Plasmodium Falciparum Malaria (Drug Resistant)	October 4, 2018	Phase 4
NCT00367653	Pfizer	Malaria	November 2006	Phase 3
NCT00274235	Institut de Recherche pour le Developpement\|National Malaria Control Program, Benin\|Ministry of Foreign Affairs, France\|Institut des Sciences Biomédicales Appliquées, Bénin\|Faculté des Sciences de la Santé, Bénin	Malaria	July 2005	Phase 3
NCT01144702	Oswaldo Cruz Foundation\|Pan American Health Organization\|Ministry of Health, Brazil\|University of Sao Paulo	Falciparum Malaria	November 2010	Phase 2\|Phase 3
NCT00158574	London School of Hygiene and Tropical Medicine\|University of Copenhagen\|National Institute for Medical Research, Tanzania\|Kilimanjaro Christian Medical Centre, Tanzania	Malaria	January 2005	Phase 2\|Phase 3
NCT00493363	University of Oxford\|World Health Organization\|NCHADS - Ministry of Health of Cambodia\|Mahidol University\|Institut Pasteur\|FHI 360\|Li Ka Shing Foundation	Falciparum Malaria	June 2007	Not Applicable
NCT02084602	Instituto Nacional de Salud. Peru\|U.S. Naval Medical Research Unit No.6 (NAMRU-6)	Malaria, Falciparum	June 18, 2014	Phase 4
NCT02488902	U.S. Army Medical Research and Development Command\|SmithKline Beecham	Malaria	August 1998	Phase 2
NCT02612545	National Institute of Allergy and Infectious Diseases (NIAID)\|National Institutes of Health Clinical Center (CC)	Acute Falciparum Malaria	November 20, 2015	Phase 1
NCT01659281	Armed Forces Research Institute of Medical Sciences, Thailand	Plasmodium Falciparum Malaria	September 2007	Not Applicable
NCT00931697	Treague Ltd\|Medicines for Malaria Venture	Healthy Subjects	June 2009	Phase 1
NCT00164216	Centers for Disease Control and Prevention\|National Institute of Health, Peru	Malaria Falciparum	March 2005
NCT00970879	Institut de Recherche pour le Developpement\|Sidaction\|Saint Antoine University Hospital\|National University Hospital, Cotonou\|Université d´Abomey-Calavi\|Ministry of Health, Benin	Malaria in Pregnancy\|HIV Infections	December 2009	Phase 3
NCT03893097	Institute of Tropical Medicine, Belgium\|Institut de Recherche en Santé, de Surveillance �pidémiologique et de Formation (IRESSEF)	Schistosoma Haematobium\|Schistosoma Mansoni	October 14, 2019	Phase 3
NCT00082576	Pfizer	Malaria, Falciparum	June 2004	Phase 2\|Phase 3
NCT01430351	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Glioblastoma\|Gliosarcoma\|Supratentorial Glioblastoma	September 14, 2011	Phase 1
NCT00373607	Institute of Tropical Medicine, Belgium	Malaria	July 2003	Phase 3
NCT00127998	Centers for Disease Control and Prevention\|Malaria Research and Training Center, Bamako, Mali	Malaria	July 2005	Not Applicable
NCT02324738	University of Oxford	Healthy	January 2015	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 120.55 mM ; Need ultrasonic)

H ₂ O : 2.86 mg/mL ( 6.90 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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
2.

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
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: 2.5 mg/mL (6.03 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

Synonyms

4-Quinolinemethanol, α-(2R)-2-piperidinyl-2,8-bis(trifluoromethyl)-, hydrochloride (1:1), (αS)-rel-

4-Quinolinemethanol, α-2-piperidinyl-2,8-bis(trifluoromethyl)-, monohydrochloride, (R*,S*)-(±)-

4-Quinolinemethanol, α-(2R)-2-piperidinyl-2,8-bis(trifluoromethyl)-, monohydrochloride, (αS)-rel-

Mefloquine hydrochloride

WR 142490

4-Quinolinemethanol, α-2-piperidinyl-2,8-bis(trifluoromethyl)-, monohydrochloride, (R*,S*)-

Loriam

Ro 21-5998/001

NSC 157387

Mefloquin hydrochloride

(±)-Mefloquine hydrochloride