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[CAS NO. 51773-92-3] Mefloquinehydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-17437A |
| Brand: | MCE |
| CAS: | 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 |
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
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)
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 |
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.
- [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.
- [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.
- [4] Rafael Pacheco-Costa, et al. Reversal of loss of bone mass in old mice treated with mefloquine. Bone. 2018 Sep;114:22-31.
Synonyms
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