1. Anti-infection Autophagy Membrane Transporter/Ion Channel Protein Tyrosine Kinase/RTK
  2. Parasite Autophagy SARS-CoV Potassium Channel ROS Kinase
  3. Mefloquine

Mefloquine  (Synonyms: Mefloquin)

目录号: HY-17437 纯度: 99.96%
COA 产品使用指南

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

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Mefloquine Chemical Structure

Mefloquine Chemical Structure

CAS No. : 53230-10-7

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     可免费申领三个不同产品的试用装。

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5 mg ¥625
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10 mg ¥1095
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25 mg ¥2300
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50 mg ¥4058
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Customer Review

Other Forms of Mefloquine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BHK-21 CC50
20.44 μM
Compound: 41
Cytotoxicity against BHK21 cells after 24 to 48 hrs by CCK8 assay
Cytotoxicity against BHK21 cells after 24 to 48 hrs by CCK8 assay
[PMID: 31549836]
Erythrocyte IC50
0.014 μM
Compound: Mefloquine
Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay
Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay
[PMID: 36561069]
HepG2 IC50
> 2000 ng/mL
Compound: Mefloquine
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 24139941]
HepG2 IC50
> 2000 ng/mL
Compound: Mefloquine
Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay
Antimalarial activity against liver stage Plasmodium berghei ANKA sporozoites infected in human HepG2 cells after 48 hrs by luciferase reporter gene assay
[PMID: 24139941]
HepG2 IC50
11.5 μM
Compound: Mefloquine
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence assay
[PMID: 36561069]
HepG2 CC50
11.8 μM
Compound: Mfq
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by alamar blue assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by alamar blue assay
[PMID: 27667552]
HepG2 EC50
9.8 μM
Compound: Mefloquine
Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay
[PMID: 29800827]
L6 IC50
4.5 μM
Compound: MQ
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay
[PMID: 25195945]
Splenocyte IC50
9.5 μM
Compound: Mfq
Cytotoxicity against BALB/c mouse splenocytes assessed as [3H]-thymidine incorporation after 24 hrs by beta-radiation counting analysis relative to control
Cytotoxicity against BALB/c mouse splenocytes assessed as [3H]-thymidine incorporation after 24 hrs by beta-radiation counting analysis relative to control
[PMID: 24530492]
U-251 IC50
10 μM
Compound: 80
Antiproliferative activity against human U251 cells by MTT assay
Antiproliferative activity against human U251 cells by MTT assay
[PMID: 30583248]
Vero CC50
212 μM
Compound: Mefloquine
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by XTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by XTT assay
[PMID: 28068604]
体外研究
(In Vitro)

Mefloquine selectively inhibits prostate cancer (PCa) cell growth with an IC50 of ~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 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

378.31

Formula

C17H16F6N2O

CAS 号
性状

固体

颜色

White to off-white

中文名称

甲氟喹

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 200 mg/mL (528.67 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6433 mL 13.2167 mL 26.4333 mL
5 mM 0.5287 mL 2.6433 mL 5.2867 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (13.22 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (13.22 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6433 mL 13.2167 mL 26.4333 mL 66.0834 mL
5 mM 0.5287 mL 2.6433 mL 5.2867 mL 13.2167 mL
10 mM 0.2643 mL 1.3217 mL 2.6433 mL 6.6083 mL
15 mM 0.1762 mL 0.8811 mL 1.7622 mL 4.4056 mL
20 mM 0.1322 mL 0.6608 mL 1.3217 mL 3.3042 mL
25 mM 0.1057 mL 0.5287 mL 1.0573 mL 2.6433 mL
30 mM 0.0881 mL 0.4406 mL 0.8811 mL 2.2028 mL
40 mM 0.0661 mL 0.3304 mL 0.6608 mL 1.6521 mL
50 mM 0.0529 mL 0.2643 mL 0.5287 mL 1.3217 mL
60 mM 0.0441 mL 0.2203 mL 0.4406 mL 1.1014 mL
80 mM 0.0330 mL 0.1652 mL 0.3304 mL 0.8260 mL
100 mM 0.0264 mL 0.1322 mL 0.2643 mL 0.6608 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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