2. Membrane Transporter/Ion Channel Anti-infection Stem Cell/Wnt TGF-beta/Smad
  3. Potassium Channel Parasite PKA
  4. Tetramisole

Tetramisole 是一种口服有效、选择性的内向整流钾通道激动剂，对 Kir2.1 亚基的 EC50 约为 30 μM。Tetramisole 还是一种抗线虫剂，可非竞争性去极化阻断神经肌肉传递。Tetramisole 促进 Kir2.1 通道的正向转运、超极化静息电位 (RP)、缩短动作电位时程 (APD)，抑制细胞内钙超载及 PKA 信号通路，发挥抗心律失常和抗心肌重塑活性。Tetramisole 可用于心脏电生理研究心肌缺血、心力衰竭相关的研究。

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Tetramisole Chemical Structure

Tetramisole Chemical Structure

CAS No. : 5036-02-2

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Tetramisole 的其他形式现货产品:

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Tetramisole 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

Tetramisole is an orally active, selective inward rectifier potassium channel agonist with an EC50 of approximately 30 μM for the Kir2.1 subunit. Tetramisole is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure[1][2].

IC50 & Target

Kir2.1

30 μM (EC50)

体外研究
(In Vitro)

Tetramisole (1-100 μM) 在全细胞膜片钳实验中，呈浓度依赖性增强大鼠心室肌细胞 (ARVMs) 的内向整流钾电流，超极化静息电位 (RP) 并缩短动作电位时程 (APD90)，且对 L 型钙电流 (ICa-L)、钠电流 (INa) 等其他离子通道无显著影响[1]。
Tetramisole (10-30 μM；24 h) 在 H9c2(2-1) 心肌细胞钙成像实验中，显著抑制异丙肾上腺素 (Iso) 诱导的细胞内钙超载，该作用可被 IK1 通道阻滞剂 BaCl2 逆转[1]。
Tetramisole (30 μM；48 h) 可上调 H9c2(2-1) 细胞中 Kir2.1 的表达水平[1]。

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

Tetramisole 相关抗体:

Western Blot Analysis[1]

Cell Line: H9c2(2-1) cardiomyocytes
Concentration: 1, 10, 30, 100 μmol/L
Incubation Time: 48 h
Result: Upregulated the expression of Kir2.1 channel and its regulatory protein SAP97 in a dose-dependent manner, with the maximum effect at 30 μmol/L (56.6% increase in Kir2.1 and 57.2% increase in SAP97 compared to control).
Reversed Iso-induced downregulation of Kir2.1 and inhibited phosphorylation of protein kinase A (p-PKA), effects that were blunted by BaCl2.
体内研究
(In Vivo)

Tetramisole (0.54 mg/kg；静脉注射；单剂量；预处理 3 分钟) 在 Sprague-Dawley 大鼠冠状动脉结扎诱导的心肌梗死模型中，显著减少室性心律失常发作次数和持续时间，降低室颤发生率，该作用可被 IK1 通道阻滞剂氯喹 (CQ) 逆转[2]。
Tetramisole (0.54 mg/kg；腹腔注射；每日 1 次；10 天) 在 Sprague-Dawley 大鼠异丙肾上腺素 (Iso) 诱导的心脏重塑模型中，改善心脏收缩功能，减轻心肌细胞肥大和间质纤维化，抑制 PKA 信号通路激活，效果依赖于 IK1 通道活性[2]。

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

Animal Model: Male Sprague-Dawley rats (2 months old, weight not specified) + coronary ligation-induced acute myocardial infarction model[2]
Dosage: 0.18, 0.54, 1.8 mg/kg
Administration: Intravenous injection 3 minutes before coronary artery occlusion; single dose
Result: Significantly reduced premature ventricular contractions (PVC) from 134 to 16 episodes, shortened ventricular tachycardia (VT) duration from 59.4 s to 8.1 s, and eliminated ventricular fibrillation (VF) (duration 0 s, incidence 0%), compared to control.
These anti-arrhythmic effects were largely reversed by co-administration of chloroquine (7.5 μg/kg), an IK1 antagonist. Pretreatment for 10 days (0.54 mg/kg/day) also reduced VT duration (42.7 s to 6.5 s) and abolished VF, associated with upregulated Kir2.1 protein expression in ventricular tissue.
Animal Model: Male Sprague-Dawley rats (2 months old, weight not specified) + isoproterenol (3 mg/kg/day, i.p., 10 days)-induced cardiac remodeling model[2]
Dosage: 0.54 mg/kg/day
Administration: Intraperitoneal injection once daily for 10 days
Result: Prevented Iso-induced increases in interventricular septum thickness and left ventricular wall thickness, normalized left ventricular ejection fraction (EF) and fractional shortening (FS), and reduced myocardial cell cross-sectional area by 22% compared to Iso group.
Masson's trichrome staining showed a 35% reduction in interstitial fibrosis, accompanied by downregulated phosphorylated PKA (p-PKA) and upregulated Kir2.1/SAP97 signaling.
Co-administration of chloroquine abolished these protective effects, confirming dependence on IK1 channel activation.
分子量

204.29

Formula

C11H12N2S
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

Tetramisole 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Tetramisole5036-02-2Potassium ChannelParasitePKAKcsAProtein kinase Aantinematodalnon-competitive depolarizingInhibitorinhibitorinhibit

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