1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. E-4031

E-4031 是一种选择性 hERG 钾通道阻断剂,可用于 III 类抗心律失常研究。

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E-4031 Chemical Structure

E-4031 Chemical Structure

CAS No. : 113559-13-0

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥748
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1 mg ¥318
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5 mg ¥700
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10 mg ¥1200
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50 mg ¥4300
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

E-4031 is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
89 nM
Compound: E-4031
Inhibition of human ERG expressed in CHO cells assessed as reduction in channel current at holding potential of 0 mV by electrophysiological method
Inhibition of human ERG expressed in CHO cells assessed as reduction in channel current at holding potential of 0 mV by electrophysiological method
[PMID: 25557493]
CHO IC50
89 nM
Compound: E-4031
Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay
Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay
[PMID: 24805037]
HEK293 IC50
0.02 μM
Compound: 1, E-4031
Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method
Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.02 μM
Compound: 1, E-4031
Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.25 μM
Compound: 1, E-4031
Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
0.69 μM
Compound: 1, E-4031
Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
2.95 μM
Compound: 1, E-4031
Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
HEK293 IC50
6.78 μM
Compound: 1, E-4031
Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
体外研究
(In Vitro)

E-4031 (0.1 ~ 10 μM) 对新西兰白兔单个 SAN 细胞的最大舒张电位 (MDP) 有显著的去极化作用,使 MDP 去极化的动作电荷在 1 μM 时从 -58.8±0.9 mV 延长至 -24.5±1.8 mV,在 10 μM 时从 -58.2±2.1 延长至 -19.6±1.8 mV[2]
E-4031 (0.1 ~ 10 μM) 能以剂量依赖的方式阻断去极化过程中的部分向外电流和随后复极化过程中的尾电流 (ITD),在新西兰白兔单个 SAN 细胞 10 μM 时,可使 ITD 降低 88% [sup] [2]。

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

分子量

474.44

Formula

C21H29Cl2N3O3S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : ≥ 50 mg/mL (105.39 mM)

* "≥" 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 2.1077 mL 10.5387 mL 21.0775 mL
5 mM 0.4215 mL 2.1077 mL 4.2155 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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 100 mg/mL (210.77 mM); 澄清溶液; 超声助溶

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
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.40%

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, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.1077 mL 10.5387 mL 21.0775 mL 52.6937 mL
5 mM 0.4215 mL 2.1077 mL 4.2155 mL 10.5387 mL
10 mM 0.2108 mL 1.0539 mL 2.1077 mL 5.2694 mL
15 mM 0.1405 mL 0.7026 mL 1.4052 mL 3.5129 mL
20 mM 0.1054 mL 0.5269 mL 1.0539 mL 2.6347 mL
25 mM 0.0843 mL 0.4215 mL 0.8431 mL 2.1077 mL
30 mM 0.0703 mL 0.3513 mL 0.7026 mL 1.7565 mL
40 mM 0.0527 mL 0.2635 mL 0.5269 mL 1.3173 mL
50 mM 0.0422 mL 0.2108 mL 0.4215 mL 1.0539 mL
60 mM 0.0351 mL 0.1756 mL 0.3513 mL 0.8782 mL
80 mM 0.0263 mL 0.1317 mL 0.2635 mL 0.6587 mL
100 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5269 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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Inquiry Information

产品名称:
E-4031
目录号:
HY-15551
需求量: