Tetramisole
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.
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- CAS 番号: 5036-02-2
- 分子式: C11H12N2S
- 分子量:204.29
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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Kir2.1 30 μM (EC50) |
Tetramisole (1-100 μM) enhances the inward rectifier potassium current in rat ventricular myocytes (ARVMs) in a concentration-dependent manner in whole-cell patch clamp experiments, hyperpolarizes the resting potential (RP) and shortens the action potential duration (APD90), but has no significant effect on other ion channels such as L-type calcium current (ICa-L) and sodium current (INa)[1].
Tetramisole (10-30 μM; 24 h) significantly inhibits isoproterenol (Iso)-induced intracellular calcium overload in H9c2(2-1) cardiomyocyte calcium imaging experiments, an effect that can be reversed by the IK1 channel blocker BaCl2[1].
Tetramisole (30 μM; 48 h) upregulates the expression level of Kir2.1 in H9c2(2-1) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H9c2(2-1) cardiomyocytes
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Concentration:1, 10, 30, 100 μmol/L
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Incubation Time:48 h
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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.
Tetramisole (0.54 mg/kg; intraperitoneal injection; once a day; 10 days) improves cardiac contractile function, reduces cardiomyocyte hypertrophy and interstitial fibrosis, and inhibits the activation of the PKA signaling pathway in the Sprague-Dawley rat model of isoproterenol (Iso)-induced cardiac remodeling, and the effect is dependent on the IK1 channel activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (2 months old, weight not specified) + coronary ligation-induced acute myocardial infarction model[2]
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Dosage:0.18, 0.54, 1.8 mg/kg
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Administration:Intravenous injection 3 minutes before coronary artery occlusion; single dose
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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.
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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]
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Dosage:0.54 mg/kg/day
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Administration:Intraperitoneal injection once daily for 10 days
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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.
化学情報
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CAS 番号 5036-02-2
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分子量 204.29
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分子式 C11H12N2S
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SMILES
C12=NC(C3=CC=CC=C3)CN1CCS2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Liu Q, et al. Tetramisole is a new IK1 channel agonist and exerts IK1 -dependent cardioprotective effects in rats. Pharmacol Res Perspect. 2022 Aug;10(4):e00992. [Content Brief]
[2]. Nowak LG, et al. Tetramisole and Levamisole Suppress Neuronal Activity Independently from Their Inhibitory Action on Tissue Non-specific Alkaline Phosphatase in Mouse Cortex. Subcell Biochem. 2015;76:239-81. [Content Brief]
Calculators
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