Tetramisole

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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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Tetramisole Chemical Structure

CAS No. : 5036-02-2

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Other In-stock Forms of Tetramisole:

Tetramisole hydrochloride

Other Forms of Tetramisole:

Tetramisole hydrochloride In-stock
Dexamisole Get quote
Levamisole Get quote

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

Kir2.1

30 μM (EC₅₀)

In Vitro

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 (I_Ca-L) and sodium current (I_Na)^[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 I_K1 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.

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.

In Vivo

Tetramisole (0.54 mg/kg; intravenous injection; single dose; 3 minutes pretreatment) significantly reduces the number and duration of ventricular arrhythmias and the incidence of ventricular fibrillation in the Sprague-Dawley rat model of myocardial infarction induced by coronary artery ligation, and this effect is reversed by the I_K1 channel blocker chloroquine (CQ)^[2].
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 I_K1 channel activity^[2].

MedChemExpress (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 I_K1 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 I_K1 channel activation.

Molecular Weight

204.29

Formula

C₁₁H₁₂N₂S

CAS No.

5036-02-2

SMILES

C12=NC(C3=CC=CC=C3)CN1CCS2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

Tetramisole Related Classifications

Infection Cardiovascular Disease

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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:

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

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