| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Pilsicainide targets cardiac sodium channels, blocking the fast inward sodium current responsible for the rapid depolarization phase of the cardiac action potential. As a class Ic antiarrhythmic agent, it exhibits intermediate kinetics of sodium channel blockade. By inhibiting sodium channels, it slows conduction velocity and increases the effective refractory period, thereby suppressing abnormal electrical activity in the heart.
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| ln Vitro |
With an IC50 of 29.2 ± 22.9 μg/mL cells, piscicaine hydrochloride (SUN-1165) (10-200 μg/mL) dose-dependently decreases the peak amplitude of net inward current in the atria of rats treated with levothyroxine (T4) [1].
Pilsicainide shortens action potential duration in canine Purkinje fibers and increases the ratio of the effective refractory period to the duration of action potential in guinea pig atrial muscle strips. Its activity as a sodium channel blocker has been confirmed in various electrophysiological assays. It is a relatively pure cardiac sodium channel blocker with minimal effects on other ion channels. |
| ln Vivo |
In rats treated with T4, atrial conduction velocity is decreased by pisicainide hydrochloride (SUN-1165) (2 mg/kg; IV; once) through a decrease in net inward current and maximal dV/dt [1].
Pilsicainide is effective in vivo for the treatment of supraventricular and ventricular arrhythmias. It is administered orally and is used clinically in Japan and other countries. Its efficacy in suppressing arrhythmias has been demonstrated in clinical studies. However, it occasionally causes QT prolongation, which is a known side effect of class Ic antiarrhythmic agents. |
| Enzyme Assay |
The primary in vitro assay for Pilsicainide is electrophysiological recording using the patch-clamp or voltage-clamp technique. Cardiac sodium channels are expressed in cells or studied in native cardiac myocytes, and the compound's ability to block sodium currents is measured. Its effects on action potential parameters, such as duration and refractory period, are assessed using microelectrode recordings in isolated cardiac tissue preparations.
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| Cell Assay |
In vitro cellular experiments for Pilsicainide involve treating cardiac myocytes or cells expressing sodium channels with the compound and measuring its effects on sodium channel activity and action potential parameters. The inhibition of sodium currents is measured using patch-clamp techniques. The effects on action potential duration and refractory period are assessed using microelectrode recordings.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats, weighing 200 to 220 g, treated with levothyroxine (T4) [1]
Doses: 2 mg/kg Route of Administration: bolus injection into the right external jugular vein within 2 minutes , primary Experimental Results: Experimental Results:QT interval was Dramatically prolonged at 15 minutes and 60 minutes after administration. The duration of P wave and QRS wave was Dramatically shortened. Action potential amplitude (APA) and maximum dV/dt were Dramatically diminished, and action potential duration was Dramatically prolonged. In vivo animal experiments for Pilsicainide involve administering the compound to animal models of cardiac arrhythmias to assess its antiarrhythmic efficacy. Its effects on arrhythmia induction, heart rate, and electrocardiogram parameters are assessed. Its pharmacokinetic properties, such as oral bioavailability and half-life, are also determined. |
| ADME/Pharmacokinetics |
Pilsicainide HCl has a molecular weight of 308.85 g/mol and a molecular formula of C17H25ClN2O. It is administered orally and is well absorbed from the gastrointestinal tract. The compound is typically stored at temperatures below 0°C. It is soluble in water and organic solvents. Its pharmacokinetic properties have been characterized in clinical studies.
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| Toxicity/Toxicokinetics |
Pilsicainide HCl is a prescription drug with a well-established safety profile. Common adverse effects may include dizziness, headache, and gastrointestinal disturbances. It occasionally causes QT prolongation, which can increase the risk of arrhythmias. It is contraindicated in patients with severe heart failure, significant bradycardia, or known hypersensitivity to the drug.
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| References | |
| Additional Infomation |
Pilsicainide hydrochloride (SUN 1165) is a class Ic antiarrhythmic agent that acts as a pure sodium channel blocker. It is used for the treatment of supraventricular and ventricular arrhythmias. The compound is available as a pharmaceutical product in some countries and is also used as a research reagent.
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| Molecular Formula |
C17H25CLN2O
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|---|---|
| Molecular Weight |
308.85
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| Exact Mass |
326.176
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| CAS # |
88069-49-2
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| Related CAS # |
Pilsicainide;88069-67-4
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| PubChem CID |
114817
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| Appearance |
White to off-white solid powder
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| Boiling Point |
416.9ºC at 760 mmHg
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| Melting Point |
212-214°
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| Flash Point |
205.9ºC
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| LogP |
3.271
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
348
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NZOSVDHCTCLGEB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H24N2O.ClH/c1-13-6-3-7-14(2)16(13)18-15(20)12-17-8-4-10-19(17)11-5-9-17;/h3,6-7H,4-5,8-12H2,1-2H3,(H,18,20);1H
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| Chemical Name |
N-(2,6-dimethylphenyl)-2-(1,2,3,5,6,7-hexahydropyrrolizin-8-yl)acetamide;hydrochloride
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| Synonyms |
SUN-1165 SUN 1165 Pilsicainide hydrochloride
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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 | 3.2378 mL | 16.1891 mL | 32.3782 mL | |
| 5 mM | 0.6476 mL | 3.2378 mL | 6.4756 mL | |
| 10 mM | 0.3238 mL | 1.6189 mL | 3.2378 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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