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  4. Kv1.5-IN-1

Kv1.5-IN-1是一种Kv1.5通道抑制剂。它在离体大鼠模型中被评估了靶点选择性和药效学作用。Kv1.5-IN-1在R5位置引入甲氧基后，其抑制效力与未取代的化合物相似。它对hKv1.5通道的IC50值为0.51μM。Kv1.5-IN-1展现了高度的选择性，比化合物Ik高出近2600倍，比化合物IId高出300倍，表明它可能是一种安全的抑制剂。由于其良好的药理学行为，Kv1.5-IN-1值得进行进一步的药效学和药代动力学评估。这些特性使Kv1.5-IN-1成为一种有潜力的Kv1.5通道抑制剂，可能在相关疾病的抑制中具有应用前景。

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Kv1.5-IN-1 Chemical Structure

Kv1.5-IN-1 Chemical Structure

CAS No. : 1469902-72-4

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Kv1.5-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Kv1.5-IN-1 is a Kv1.5 channel inhibitor. Its target selectivity and pharmacodynamic effects were evaluated in an in vitro rat model. After the introduction of a methoxy group at the R5 position, Kv1.5-IN-1 showed inhibitory potency similar to that of the unsubstituted compound. Its IC50 value for hKv1.5 channels was 0.51 μM. Kv1.5-IN-1 exhibited a high degree of selectivity, nearly 2,600 times higher than compound Ik and 300 times higher than compound IId, indicating that it may be a safe inhibitor. Due to its good pharmacological behavior, Kv1.5-IN-1 deserves further pharmacodynamic and pharmacokinetic evaluation. These properties make Kv1.5-IN-1 a potential Kv1.5 channel inhibitor that may have application prospects in the treatment of related diseases.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
418.35 μM
Compound: IIIl
Inhibition of human ERG channel expressed in CHO cells by whole cell patch clamp technique
Inhibition of human ERG channel expressed in CHO cells by whole cell patch clamp technique
[PMID: 24071446]
HEK293 IC50
0.51 μM
Compound: IIIl
Inhibition of human Kv1.5 channel expressed in HEK293 cells by whole cell patch clamp technique
Inhibition of human Kv1.5 channel expressed in HEK293 cells by whole cell patch clamp technique
[PMID: 24071446]
Ventricular myocyte IC50
52.6 μM
Compound: IIIl
Inhibition of sodium channel in guinea pig ventricular myocytes by whole cell patch clamp technique
Inhibition of sodium channel in guinea pig ventricular myocytes by whole cell patch clamp technique
[PMID: 24071446]
分子量

510.99

Formula

C25H23ClN4O4S
CAS 号
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

Kv1.5-IN-1 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

Kv1.5-IN-11469902-72-4OthersInhibitorinhibitorinhibit

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