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M2319 Sigma

Mefloquine hydrochloride

≥98% (HPLC), powder

Synonym: (AS)-rel-a-(2R)-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol monohydrochloride

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Description

Biochem/physiol Actions

Blocker of gap junction channels Cx36 and Cx50.

Features and Benefits

This compound was developed by Merck. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

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European Pharmacopoeia (EP) Reference Standard

Safety & Documentation

Safety Information

Symbol 
GHS07  GHS07
Signal word 
Warning
Hazard statements 
Personal Protective Equipment 
WGK Germany 
3
RTECS 
VC0308000

Documents

Certificate of Analysis

Certificate of Origin

Protocols & Articles

Peer-Reviewed Papers

References

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Potent block of Cx36 and Cx50 gap junction channels by mefloquine. Cruikshank, S.J., et al. Proc. Natl. Acad. Sci. U. S. A. 101, 12364-12369, (2004)

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Defining the timing of action of antimalarial drugs against Plasmodium falciparum. Wilson DW, Langer C, Goodman CD, et al. Antimicrob. Agents Chemother. 57(3), 1455-67, (2013)

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Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development. Zaloumis S, Humberstone A, Charman SA, et al. Malaria Journal 11, 303, (2012)

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Lysosomal disruption preferentially targets acute myeloid leukemia cells and progenitors. Sukhai MA, Prabha S, Hurren R, et al. J. Clin. Invest. 123(1), 315-28, (2013)

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Efficacy of mefloquine intermittent preventive treatment in pregnancy against Schistosoma haematobium infection in Gabon: a nested randomized controlled assessor-blinded clinical trial. Basra A, Mombo-Ngoma G, Melser MC, et al. Clin. Infect. Dis. 56(6), e68-75, (2013)

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The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives. Tukulula M, Little S, Gut J, et al. Eur. J. Med. Chem. 57, 259-67, (2012)

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Histamine induces ATP release from human subcutaneous fibroblasts, via pannexin-1 hemichannels, leading to Ca2+ mobilization and cell proliferation. Pinheiro AR, Paramos-de-Carvalho D, Certal M, et al. J. Biol. Chem. 288(38), 27571-83, (2013)

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Drugs for treating urinary schistosomiasis. Kramer CV, Zhang F, Sinclair D, et al. Cochrane Database Syst. Rev. 8, CD000053, (2014)

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The use of a prodrug approach to minimize potential CNS exposure of next generation quinoline methanols while maintaining efficacy in in vivo animal models. Sousa JC, Milner E, Carroll D, et al. Eur. J. Drug Metab. Pharmacokinet. 39(4), 231-6, (2014)

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Schizontemia as an indicator of severe malaria. Tangpukdee N, Krudsood S, and Wilairatana P Southeast Asian J. Trop. Med. Public Health 44(5), 740-3, (2013)

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Effect of single nucleotide polymorphisms in cytochrome P450 isoenzyme and N-acetyltransferase 2 genes on the metabolism of artemisinin-based combination therapies in malaria patients from Cambodia and Tanzania. Staehli Hodel EM, Csajka C, Ariey F, et al. Antimicrob. Agents Chemother. 57(2), 950-8, (2013)

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[New combination therapy against malaria]. Holtermann MK Tidsskr. Nor. Laegeforen. 132(15), 1741, (2012)

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Artemisinin-resistant Plasmodium falciparum in Pursat province, western Cambodia: a parasite clearance rate study. Amaratunga C, Sreng S, Suon S, et al. Lancet Infect. Dis. 12(11), 851-8, (2012)

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Malaria. White NJ, Pukrittayakamee S, Hien TT, et al. Lancet 383(9918), 723-35, (2014)

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Efficacy of dihydroartemisinin-piperaquine for treatment of uncomplicated Plasmodium falciparum and Plasmodium vivax in Cambodia, 2008 to 2010. Leang R, Barrette A, Bouth DM, et al. Antimicrob. Agents Chemother. 57(2), 818-26, (2013)

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First case of Plasmodium knowlesi infection in a Japanese traveller returning from Malaysia. Tanizaki R, Ujiie M, Kato Y, et al. Malaria Journal 12, 128, (2013)

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Treatment of suspected hyper-reactive malarial splenomegaly (HMS) in pregnancy with mefloquine. Jaroensuk J, Stoesser N, Leimanis ML, et al. Am. J. Trop. Med. Hyg. 90(4), 609-11, (2014)

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Humanized mouse model of glucose 6-phosphate dehydrogenase deficiency for in vivo assessment of hemolytic toxicity. Rochford R, Ohrt C, Baresel PC, et al. Proc. Natl. Acad. Sci. U. S. A. 110(43), 17486-91, (2013)

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Artemisinin resistance containment project in Thailand. II: Responses to mefloquine-artesunate combination therapy among falciparum malaria patients in provinces bordering Cambodia. Satimai W, Sudathip P, Vijaykadga S, et al. Malaria Journal 11, 300, (2012)

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Preliminary investigation of the contribution of CYP2A6, CYP2B6, and UGT1A9 polymorphisms on artesunate-mefloquine treatment response in Burmese patients with Plasmodium falciparum malaria. Phompradit P, Muhamad P, Cheoymang A, et al. Am. J. Trop. Med. Hyg. 91(2), 361-6, (2014)

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The story of artesunate-mefloquine (ASMQ), innovative partnerships in drug development: case study. Wells S, Diap G, and Kiechel JR Malaria Journal 12, 68, (2013)

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Favourable outcome of progressive multifocal leukoencephalopathy with mefloquine treatment in combination with antiretroviral therapy in an HIV-infected patient. Adachi E, Koibuchi T, Imai K, et al. Int. J. STD AIDS 23(8), 603-5, (2012)

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Cell type-specific, presynaptic LTP of inhibitory synapses on fast-spiking GABAergic neurons in the mouse visual cortex. Sarihi A, Mirnajafi-Zadeh J, Jiang B, et al. J. Neurosci. 32(38), 13189-99, (2012)

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Efficacy and tolerability of a new formulation of artesunate-mefloquine for the treatment of uncomplicated malaria in adult in Senegal: open randomized trial. Tine RC, Faye B, Sylla K, et al. Malaria Journal 11, 416, (2012)

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Primaquine for reducing Plasmodium falciparum transmission. Graves PM, Gelband H, and Garner P Cochrane Database Syst. Rev. 9, CD008152, (2012)

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Chemosensitization potential of P-glycoprotein inhibitors in malaria parasites. Alcantara LM, Kim J, Moraes CB, et al. Exp. Parasitol. 134(2), 235-43, (2013)

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Investigation of the in vitro gender-specific partitioning of mefloquine in malarial infected red blood cells and plasma. Seethorn N, Wernsdorfer WH, Noedl H, et al. Am. J. Trop. Med. Hyg. 89(4), 737-41, (2013)

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An in vivo drug screening model using glucose-6-phosphate dehydrogenase deficient mice to predict the hemolytic toxicity of 8-aminoquinolines. Zhang P, Gao X, Ishida H, et al. Am. J. Trop. Med. Hyg. 88(6), 1138-45, (2013)

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Failure of mefloquine therapy in progressive multifocal leukoencephalopathy: report of two Japanese patients without human immunodeficiency virus infection. Kobayashi Z, Akaza M, Numasawa Y, et al. J. Neurol. Sci. 324(1-2), 190-4, (2013)

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Active sulforhodamine 101 uptake into hippocampal astrocytes. Schnell C, Hagos Y, and Hülsmann S PLoS ONE 7(11), e49398, (2012)

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Mefloquine exposure induces cell cycle delay and reveals stage-specific expression of the pfmdr1 gene. Bohórquez EB, Juliano JJ, Kim HS, et al. Antimicrob. Agents Chemother. 57(2), 833-9, (2013)

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Spontaneous activity in the developing gerbil auditory cortex in vivo involves GABAergic transmission. Kotak VC, Péndola LM, and Rodríguez-Contreras A Neuroscience 226, 130-44, (2012)

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Study on the developmental toxicity of combined artesunate and mefloquine antimalarial drugs on rats. Boareto AC, Müller JC, de Araujo SL, et al. Reprod. Toxicol. 34(4), 658-64, (2012)

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The anti-malarial drug Mefloquine disrupts central autonomic and respiratory control in the working heart brainstem preparation of the rat. Lall VK, Dutschmann M, Deuchars J, et al. J. Biomed. Sci. 19, 103, (2012)

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Effects of the combined artesunate and mefloquine antimalarial drugs on rat embryos. Boareto AC, Müller JC, Lourenço EL, et al. Hum. Exp. Toxicol. 32(9), 930-41, (2013)

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Factors associated with cerebral malaria. Adhikari B, Tangpukdee N, Krudsood S, et al. Southeast Asian J. Trop. Med. Public Health 44(6), 941-9, (2013)

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Progressive Multifocal Leukoencephalopathy with Immune Reconstitution Inflammatory Syndrome (PML-IRIS): two case reports of successful treatment with mefloquine and a review of the literature. Young BE, Yeo TR, Lim HT, et al. Ann. Acad. Med. Singapore 41(12), 620-4, (2012)

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Biowaiver monographs for immediate release solid oral dosage forms: mefloquine hydrochloride. Strauch S, Jantratid E, Dressman JB, et al. J. Pharm. Sci. 100(1), 11-21, (2011)

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Merck 14,5801

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