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

Mefloquine (Mefloquin) 是一種口服有效的喹啉抗瘧藥，是一種抗 SARS-CoV-2 進(jìn)入抑制劑。Mefloquine 也是一種 K+ 通道 (KvQT1/minK) 拮抗劑，IC50 為 ~1 μM。Mefloquine 可用于瘧疾、系統(tǒng)性紅斑狼瘡和癌癥的研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Mefloquine Chemical Structure

Mefloquine Chemical Structure

CAS No. : 53230-10-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥687
In-stock
5 mg ￥625
In-stock
10 mg ￥1095
In-stock
25 mg ￥2300
In-stock
50 mg ￥4058
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Mefloquine:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

細(xì)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]
體外研究
(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.
體內(nèi)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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

甲氟喹
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 200 mg/mL (528.67 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

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

    此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

掃碼獲得
動(dòng)物溶解方案

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， PEG300/PEG400，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

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