| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In whole-cell patch-clamp experiments, tetraimidazole (1–100 μM) enhanced inward rectifier potassium currents in rat ventricular myocytes (ARVMs) in a concentration-dependent manner, hyperpolarized the resting potential (RP), and shortened the action potential duration (APD90), but had no significant effect on other ion channels such as L-type calcium currents (ICa-L) and sodium currents (INa) [1]. In H9c2(2–1) cardiomyocyte calcium imaging experiments, tetraimidazole (10–30 μM; 24 h) significantly inhibited isoproterenol (Iso)-induced intracellular calcium overload, an effect that could be reversed by the IK1 channel blocker BaCl2 [1]. Tetraimidazole (30 μM; 48 h) upregulated the expression level of Kir2.1 in H9c2(2–1) cells [1].
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| ln Vivo |
Tetraimidazole (0.54 mg/kg; intravenous injection; single dose; pretreatment for 3 minutes) significantly reduced the number and duration of ventricular arrhythmias and the incidence of ventricular fibrillation in a Sprague-Dawley rat model of myocardial infarction induced by coronary artery ligation, while the IK1 channel blocker chloroquine (CQ) reversed this effect [2]. Tetraimidazole (0.54 mg/kg; intraperitoneal injection; once daily for 10 days) improved myocardial contractile function, reduced cardiomyocyte hypertrophy and interstitial fibrosis in an isoproterenol (Iso)-induced Sprague-Dawley rat model of cardiac remodeling, and inhibited the activation of the PKA signaling pathway, and this effect was dependent on IK1 channel activity [2].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: H9c2(2-1) cardiomyocytes Tested Concentrations: 1, 10, 30, 100 μmol/L Incubation Duration: 48 hours Experimental Results: The expression of Kir2.1 channel and its regulatory protein SAP97 was upregulated in a dose-dependent manner, with the best effect at 30 μmol/L (compared to the control group, Kir2.1 increased by 56.6% and SAP97 increased by 57.2%). Iso-induced downregulation of Kir2.1 was reversed, and phosphorylation of protein kinase A (p-PKA) was inhibited, while barium chloride (BaCl2) attenuated these effects. |
| Animal Protocol |
Animal/Disease Models:Male Sprague-Dawley rats (2 months old, weight not specified) + acute myocardial infarction model induced by coronary artery ligation [2]
Doses: 0.18, 0.54, 1.8 mg/kg Route of Administration: Intravenous injection 3 minutes before coronary artery occlusion; single administration Experimental Results: Compared with the control group, ventricular premature beats (PVCs) were significantly reduced from 134 to 16, ventricular tachycardia (VT) duration was shortened from 59.4 seconds to 8.1 seconds, and ventricular fibrillation (VF) was eliminated (duration 0 seconds, incidence 0%). These antiarrhythmic effects were significantly reversed by the combined use of the IK1 antagonist chloroquine (7.5 μg/kg). Pre-treatment for 10 days (0.54 mg/kg/day) can also shorten the duration of ventricular tachycardia (from 42.7 seconds to 6.5 seconds) and eliminate ventricular fibrillation, which is related to the upregulation of Kir2.1 protein expression in ventricular tissue. Animal/Disease Models:Male Sprague-Dawley rats (2 months old, weight not specified) + isoproterenol (3 mg/kg/day, intraperitoneal injection, 10 days) induced cardiac remodeling model [2] Doses:0.54 mg/kg/day< Route of Administration:Intraperitoneal injection once daily for 10 days Experimental Results:Compared with the isoproterenol group, it prevented the increase in interventricular septal thickness and left ventricular wall thickness induced by isoproterenol, restored the left ventricular ejection fraction (EF) and fractional shortening (FS) to normal, and reduced the cross-sectional area of cardiomyocytes by 22%. Masson trichrome staining showed a 35% reduction in interstitial fibrosis, accompanied by downregulation of phosphorylated PKA (p-PKA) and upregulation of the Kir2.1/SAP97 signaling pathway. Chloroquine combination therapy eliminated these protective effects, confirming that it depends on the activation of IK1 channels. |
| References |
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| Molecular Formula |
C11H12N2S
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|---|---|
| Molecular Weight |
204.29
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| CAS # |
5036-02-2
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
C12=NC(C3=CC=CC=C3)CN1CCS2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8950 mL | 24.4750 mL | 48.9500 mL | |
| 5 mM | 0.9790 mL | 4.8950 mL | 9.7900 mL | |
| 10 mM | 0.4895 mL | 2.4475 mL | 4.8950 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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