Mefloquine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.

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.

Mefloquin hydrochloride

Autophagy

Autophagy

hemozoin

Infection

Bacterial Infection

51773-92-3

414.7731

C17H17ClF6N2O

>98% (HPLC)

10 mM in DMSO

C1CCN[C@H](C1)[C@H](C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O.Cl

4-Quinolinemethanol, α-(2R)-2-piperidinyl-2,8-bis(trifluoromethyl)-, hydrochloride (1:1), (αS)-rel-

(-20℃)

With Ice Pack

≥ 2 years