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Mefloquine hydrochloride

CAS No. : 51773-92-3

MCE 国际站：Mefloquine hydrochloride

产品活性：Mefloquine hydrochloride (Mefloquin hydrochloride) 是一种喹啉抗疟药，是一种抗 SARS-CoV-2 进入抑制剂。Mefloquine hydrochloride 也是一种 K⁺ 通道 (KvQT1/minK) 拮抗剂，IC₅₀ 为 ~1 μM。Mefloquine hydrochloride 可用于疟疾、系统性红斑狼疮和癌症的研究。

研究领域：Anti-infection  |  Autophagy  |  Membrane Transporter/Ion Channel  |  Protein Tyrosine Kinase/RTK

作用靶点：Parasite  |  SARS-CoV  |  Autophagy  |  Potassium Channel  |  ROS Kinase

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.

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