2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. Potassium Channel Sodium Channel Adrenergic Receptor
  4. hERG-IN-3

hERG-IN-3 是一种口服有效的 hERG 阻滞剂，其 IC50 为 44.5 nM。hERG-IN-3 对 β2 肾上腺素受体的 Ki 值为 14 nM。hERG-IN-3表现出骨骼肌 Nav1.4 钠通道阻断活性 (IC50 =4.4 μM，比 hNav1.5 高 3倍)。hERG-IN-3 在动物模型中显示出强大的抗肌张力活性。hERG-IN-3 可用于先天性肌强直的研究。

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hERG-IN-3

hERG-IN-3 Chemical Structure

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hERG-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Sodium Channel 亚型特异性产品:

查看所有亚型
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

查看 Adrenergic Receptor 亚型特异性产品:

查看所有亚型
α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

hERG-IN-3 is an orally active hERG blocker with an IC50 of 44.5 nM. hERG-IN-3 exhibits a Ki for β2-adrenergic receptor of 14 nM. hERG-IN-3 exhibits the skeletal muscle Nav1.4 and sodium channel-blocking activities (IC50 =4.4 μM, 3-fold increasement than hNav1.5). hERG-IN-3 displays a potent antimyotonic activity in an animal model. hERG-IN-3 can be used for the study of Myotonia Congenita[1].

IC50 & Target[1]

Beta-2 adrenergic receptor

14 nM (IC50)

α1A-adrenergic receptor

270 nM (IC50)

Nav1.4

4.4 μM (IC50)

Nav1.5

12 μM (IC50)

体外研究
(In Vitro)

hERG-IN-3 对 α1A 和 β2 受体具有亲和作用，Ki 值分别为270 nM和14 nM[1]。
hERG-IN-3 对 K+ 去极化豚鼠回肠纵向平滑肌具有松弛活性，其IC50 = 0.83 μM[1]。

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

hERG-IN-3 相关抗体:
体内研究
(In Vivo)

hERG-IN-3 (1 mg/kg, p.o., 单次给药) 显著改善大鼠肌强直模型肌肉僵硬症状[1]。

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

Animal Model: Myotonia model established in adult Wistar rats (350/500 g)[1]
Dosage: 1 mg/kg
Administration: Oral administration (p.o.), single dose
Result: The reduction of the time of righting reflex in vivo in the rat model of myotonia was observed.
分子量

429.53

Formula

C22H27N3O4S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

hERG-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

hERG-IN-3Potassium ChannelSodium ChannelAdrenergic ReceptorKcsANa channelsNa+ channelsBeta ReceptorLubeluzolehERG liabilitySodium-channel blockersUse-dependenceMyotoniaInhibitorinhibitorinhibit

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产品名称：
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目录号：
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