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Mefloquine hydrochloride is a Cx36 and Cx50 gap channel blocker (IC50 values are 0.3 and 1.1 μM, resepctively). Blocks gap junctional-coupling between interneurons in neocortical slices. Also antimalarial. Bind 80S ribosome of Plasmodium falciparum to inhibit protein synthesis. Improves survival in P berghei-infected mice. Additionally exhibits antischistosomal activity in vitro and in vivo. Exhibits antiviral activities against SARS-CoV-2 (IC50 < 10 μM).
Mefloquine hydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 414.77. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.41 mL||12.05 mL||24.11 mL|
|5 mM||0.48 mL||2.41 mL||4.82 mL|
|10 mM||0.24 mL||1.21 mL||2.41 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References are publications that support the biological activity of the product.
Pasche et al (2019) Early antischistosomal leads identified from in vitro and in vivo screening of the Medicines for Malaria Venture Pathogen Box. ACS Infect.Dis. 5 102 PMID: 30398059
Wong et al (2017) Mefloquine targets the Plasmodium falciparum 80S ribosome to inhibit protein synthesis. Nat.Microbiol. 2 17031 PMID: 28288098
Cruikshank et al (2004) Potent block of Cx36 and Cx50 gap junction channels by meflo. Proc.Natl.Acad.Sci.U.S.A. 101 12364 PMID: 15297615
Ohnmacht et al (1971) Antimalarials. 7. Bis(trifluoromethyl)-α-(2-piperidyl)-4-quinolinemethanols. J.Med.Chem. 14 926 PMID: 5115690
Jeon et al (2020) Identification of antiviral drug candidates against SARS-CoV-2 from FDA-approved drugs. Antimicrob.Agents Chemother. 64 PMID: 32366720
If you know of a relevant reference for Mefloquine hydrochloride, please let us know.
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.