Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2entry inhibitor. Mefloquine is also aK⁺channel (KvQT1/minK)antagonist with anIC₅₀of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus andcancerresearch^[1][2][3].

Mefloquine selectively inhibits prostate cancer (PCa) cell growth with an IC₅₀of ~10 μM. Mefloquine also induces hyperpolarization of the mitochondrial membrane potential (MMP), as well as ROS generation^[2].
Mefloquine (10 μM)-mediated ROS simultaneously downregulated Akt phosphorylation and activated ERK, JNK and AMPK signaling in PC3 cells^[2].
Mefloquine shows higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC₅₀of 1.28 μM, IC₉₀of 2.31 μM, and IC₉₉of 4.39 μM in VeroE6/TMPRSS2 cells. Mefloquine inhibits viral entry after viral attachment to the target cell^[3].

Mefloquine (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^[4].

378.31

C₁₇H₁₆F₆N₂O

53230-10-7

甲氟喹

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