Mefloquine hydrochloride

Pricing Availability   Qty
Description: Cx36 and Cx50 gap channel blocker; also antimalarial and antischistosomal
Chemical Name:S)-rel-α-(2R)-2-Piperidinyl-2,3-bis(trifluoromethyl-4-quinolinemethanol hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews

Biological Activity for Mefloquine hydrochloride

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).

Compound Libraries for Mefloquine hydrochloride

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.

Technical Data for Mefloquine hydrochloride

M. Wt 414.77
Formula C17H16F6N2O.HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 51773-92-3
PubChem ID 65329
InChI Key WESWYMRNZNDGBX-YLCXCWDSSA-N
Smiles [H][C@]1([C@H](C2=CC(C(F)(F)F)=NC3=C(C(F)(F)F)C=CC=C23)O)CCCCN1.Cl

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.

Solubility Data for Mefloquine hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 41.48 100
DMSO 20.74 50

Preparing Stock Solutions for Mefloquine hydrochloride

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Mefloquine hydrochloride

Certificate of Analysis / Product Datasheet
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References for Mefloquine hydrochloride

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


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Citations for Mefloquine hydrochloride

Citations are publications that use Tocris products.

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