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Submit ReviewMefloquine 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. 了解 Tocris 化合物库的更多信息。
分子量 | 414.77 |
公式 | C17H16F6N2O.HCl |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 41.48 | 100 | |
DMSO | 20.74 | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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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