Mefloquine hydrochloride

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Cat.No. 6819 - Mefloquine hydrochloride | C17H16F6N2O.HCl | CAS No. 51773-92-3
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
Literature (2)

Biological Activity

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.

Technical Data

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

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

Preparing Stock Solutions

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

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References

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


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Citations for Mefloquine hydrochloride

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