Tetramisole hydrochloride
Based on 1 Customer Validation
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.
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- Pureté: 99.04%
- CAS No.: 5086-74-8
- Formule: C11H13ClN2S
- Masse moléculaire:240.75
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Activité biologique
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Kir2.1 30 μM (EC50) |
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 (ICa-L) and sodium current (INa)[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 IK1 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.
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Cell Line:H9c2(2-1) cardiomyocytes
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Concentration:1, 10, 30, 100 μM
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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) 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 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 Tetramisole
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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 Tetramisole
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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.
Chemical Information
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CAS No. 5086-74-8
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Appearance Solid
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Masse moléculaire 240.75
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Formule C11H13ClN2S
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Color White to off-white
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SMILES
[H]Cl.C12=NC(C3=CC=CC=C3)CN1CCS2
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Synonyms
(±)-Tetramisole hydrochloride; DL-Tetramisole hydrochloride; R-829
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: PBS
Solubility: 110 mg/mL (456.91 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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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.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
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- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
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.
| 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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