1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Mexiletine

Mexiletine  (Synonyms: 美西律; KOE-1173)

目录号: HY-119521 纯度: 99.92%
COA 产品使用指南 技术支持

Mexiletine 是一种口服有效的抗心律失常剂,也被发现对肌强直和神经病理性疼痛有效。Mexiletine 通过阻断钠离子通道 (IC50 : 75±8 μM 于封闭性阻断, 23.6±2.8 μM 于使用依赖性阻断) 发挥作用,可被用于心血管与神经病学研究。

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Mexiletine Chemical Structure

Mexiletine Chemical Structure

CAS No. : 31828-71-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1510
In-stock
250 mg ¥1373
In-stock
1 g ¥3705
In-stock
5 g   询价  
10 g   询价  

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Other Forms of Mexiletine:

MCE 顾客使用本产品发表的 2 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research[1][2][3][4][5].

IC50 & Target

IC50: 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block (sodium channel of HEK293 transfected with hNav1.5 plasmid)[2]

体外研究
(In Vitro)

Mexiletine (10µM, 48 h) 在转染 SCN5A-WT 或 SCN5A-1795insD 的 HEK293A 细胞中增加了峰值 INa 和晚期 INa,Mexiletine (10µM, 5 min) 阻断了晚期 INa[3]

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

体内研究
(In Vivo)

Mexiletine (30, 100 mg/kg, 口服, 急性给药) 逆转 Oxaliplatin (HY-17371) 诱导的大鼠机械痛觉过敏和低温痛觉过敏[4]

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

Animal Model: Male Sprague-Dawley rats with Oxaliplatin (HY-17371)-induced neuropathic pain [4]
Dosage: Oxaliplatin (4 mg /kg) and Mexiletine(10, 30, 100 mg/kg)
Administration: Oxaliplatin, Intraperitoneal injection (i.p.)in days 1, 2, 8, 9, 15, 16, 22, and 23; Mexiletine, Oral gavage (p.o.), acute administration
Result: 100 mg/kg completely reversed the reduction of 50% paw withdrawal threshold by Oxaliplatin at 60 min after administration in the von Frey test, completely reversed the increase of number of withdrawal responses at 60 and 120 min after administration in the acetone test.
30 mg/kg partly reversed the symptom and 10 mg/kg did not reverse any symptom. The effect disappeared by 180 min after administration.
Clinical Trial
分子量

179.26

Formula

C11H17NO

CAS 号
性状

液体

颜色

Colorless to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -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 : ≥ 175 mg/mL (976.24 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.5785 mL 27.8924 mL 55.7849 mL
5 mM 1.1157 mL 5.5785 mL 11.1570 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:

以下溶解方案源自文献,仅供参考,建议您先取少量样品进行尝试。

  • 方案 一

    PBS

  • 方案 二

    10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline

  • 方案 三

    10% DMSO + 90% (20% SBE-β-CD in saline)

  • 方案 四

    10% DMSO + 90% corn oil

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
计算结果
工作液所需浓度 : mg/mL
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 5.5785 mL 27.8924 mL 55.7849 mL 139.4622 mL
5 mM 1.1157 mL 5.5785 mL 11.1570 mL 27.8924 mL
10 mM 0.5578 mL 2.7892 mL 5.5785 mL 13.9462 mL
15 mM 0.3719 mL 1.8595 mL 3.7190 mL 9.2975 mL
20 mM 0.2789 mL 1.3946 mL 2.7892 mL 6.9731 mL
25 mM 0.2231 mL 1.1157 mL 2.2314 mL 5.5785 mL
30 mM 0.1859 mL 0.9297 mL 1.8595 mL 4.6487 mL
40 mM 0.1395 mL 0.6973 mL 1.3946 mL 3.4866 mL
50 mM 0.1116 mL 0.5578 mL 1.1157 mL 2.7892 mL
60 mM 0.0930 mL 0.4649 mL 0.9297 mL 2.3244 mL
80 mM 0.0697 mL 0.3487 mL 0.6973 mL 1.7433 mL
100 mM 0.0558 mL 0.2789 mL 0.5578 mL 1.3946 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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Mexiletine
目录号:
HY-119521
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