Mefloquine hydrochloride

SKU: orb1224840

Description

A quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine; inhibits autophagy and has been recognized as a potential target for cancer therapy.Bacterial Infection Approved(In Vitro):Mefloquine hydrochloride selectively inhibits prostate cancer (PCa) cell growth with an IC50 of ~10 μM. Mefloquine hydrochloride also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS generation.Mefloquine hydrochloride (10 μM)-mediated ROS simultaneously downregulated Akt phosphorylation and activated ERK, JNK and AMPK signaling in PC3 cells.Mefloquine shows higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC50 of 1.28 μM, IC90 of 2.31 μM, and IC99 of 4.39 μM in VeroE6/TMPRSS2 cells. Mefloquine inhibits viral entry after viral attachment to the target cell.(In Vivo):Mefloquine hydrochloride (5 mg/kg; i.p.; daily; 14 days) reverses the lower vertebral cancellous bone volume and bone formation; and has modest effects on cortical bone volume, thickness, and moment of inertia in old mice.

Key Properties

• CAS Number: 51773-92-3
• MW: 414.7731
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₇ClF₆N₂O
• SMILES: C1CCN[C@H](C1)[C@H](C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O.Cl
• Target: Autophagy
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Mefloquine hydrochloride (5 mg/kg; i.p.; daily; 14 days) reverses the lower vertebral cancellous bone volume and bone formation; and has modest effects on cortical bone volume, thickness, and moment of inertia in old mice. Animal model: Young 3.5-month-old and old 21-month-old female C57BL/6 mice. Dosage: 5 mg/kg. Administration: Intraperitoneal injection; daily; 14 days. Result: Reversed the lower vertebral cancellous bone volume and bone formation in old mice.
• In Vitro:
  Mefloquine hydrochloride selectively inhibits prostate cancer (PCa) cell growth with an IC50 of ~10 μM. Mefloquine hydrochloride also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS generation. Mefloquine hydrochloride (10 μM)-mediated ROS simultaneously downregulated Akt phosphorylation and activated ERK, JNK and AMPK signaling in PC3 cells. Mefloquine shows higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC50 of 1.28 μM, IC90 of 2.31 μM, and IC99 of 4.39 μM in VeroE6/TMPRSS2 cells. Mefloquine inhibits viral entry after viral attachment to the target cell.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Mefloquin hydrochloride

Quick Database Links

Gene Symbol

Autophagy