Cat. No.: HY-B1194

Tetramisole hydrochloride

(Synonyms: (±)-Tetramisole hydrochloride; DL-Tetramisole hydrochloride; R-829)

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Tetramisole hydrochloride is an orally active, selective inward rectifier potassium channel agonist with an EC₅₀ of approximately 30 μM for the Kir2.1 subunit. Tetramisole hydrochloride is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole hydrochloride 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 hydrochloride can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure.

For research use only. We do not sell to patients.

Purity: 99.04%
CAS No.: 5086-74-8
Formula: C₁₁H₁₃ClN₂S
Molecular Weight:240.75

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Tetramisole hydrochloride Chemical Structure

CAS No.: 5086-74-8

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Kir2.1

30 μM (EC₅₀)

All Parasite Isoforms :

All PKA Isoforms :

In Vitro

Tetramisole hydrochloride (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 hydrochloride (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 hydrochloride (30 μM; 48 h) can upregulate 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 μM
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) hydrochloride 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) hydrochloride 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 Tetramisole
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 Tetramisole
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.

Chemical Information

CAS No. 5086-74-8
Appearance Solid
Molecular Weight 240.75
Formula C₁₁H₁₃ClN₂S
Color White to off-white
SMILES

[H]Cl.C12=NC(C3=CC=CC=C3)CN1CCS2
Synonyms

(±)-Tetramisole hydrochloride; DL-Tetramisole hydrochloride; R-829
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (415.37 mM; Need ultrasonic)

DMSO : 10 mg/mL (41.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1537 mL

20.7684 mL

41.5369 mL

5 mM

0.8307 mL

4.1537 mL

8.3074 mL

10 mM

0.4154 mL

2.0768 mL

4.1537 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (4.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1 mg/mL (4.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (4.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 110 mg/mL (456.91 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	4.1537 mL	20.7684 mL	41.5369 mL	103.8422 mL
	5 mM	0.8307 mL	4.1537 mL	8.3074 mL	20.7684 mL
	10 mM	0.4154 mL	2.0768 mL	4.1537 mL	10.3842 mL
	15 mM	0.2769 mL	1.3846 mL	2.7691 mL	6.9228 mL
	20 mM	0.2077 mL	1.0384 mL	2.0768 mL	5.1921 mL
	25 mM	0.1661 mL	0.8307 mL	1.6615 mL	4.1537 mL
	30 mM	0.1385 mL	0.6923 mL	1.3846 mL	3.4614 mL
	40 mM	0.1038 mL	0.5192 mL	1.0384 mL	2.5961 mL
H₂O	50 mM	0.0831 mL	0.4154 mL	0.8307 mL	2.0768 mL
	60 mM	0.0692 mL	0.3461 mL	0.6923 mL	1.7307 mL
	80 mM	0.0519 mL	0.2596 mL	0.5192 mL	1.2980 mL
	100 mM	0.0415 mL	0.2077 mL	0.4154 mL	1.0384 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Tetramisole hydrochloride

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All Parasite Isoforms

All PKA Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tetramisole hydrochloride Related Classifications

HY-B1194 Related Classifications