Ibutilide: Mechanism, Uses & Lab FAQs
Ibutilide: Mechanism, Uses & Lab FAQs
Ibutilide is a class III antiarrhythmic compound widely used in cardiovascular research to selectively block rapid delayed rectifier potassium currents (IKr) and activate slow inward sodium currents, thereby prolonging cardiac action potential duration and refractoriness.
- Chemical Class
- Class III antiarrhythmic agent (methanesulfonanilide derivative)
- Primary Mechanism
- IKr (hERG channel) blockade and activation of slow inward Na⁺ current, prolonging action potential duration
- Research Application
- Cardiac electrophysiology studies, atrial fibrillation and flutter models, ion channel pharmacology
- Solubility
- Soluble in DMSO and ethanol; limited aqueous solubility at physiological pH
- Storage Recommendation
- Store at -20 °C, protected from light and moisture, in a tightly sealed container
- CAS Number
- 122647-31-8
What Is Ibutilide and How Does It Work?
Ibutilide is a methanesulfonanilide-class compound classified as a class III antiarrhythmic agent. Its predominant mechanism of action involves blockade of the rapid delayed rectifier potassium channel (IKr, encoded by the hERG gene), which is a critical repolarizing current in cardiac myocytes. Unlike many other class III agents, ibutilide also activates a slow, sustained inward sodium current, further delaying repolarization.
The combined effect of IKr blockade and enhanced inward Na⁺ current prolongs the cardiac action potential duration (APD) and the effective refractory period (ERP) in both atrial and ventricular tissue. This makes ibutilide a valuable pharmacological tool for researchers studying cardiac electrophysiology, repolarization dynamics, and arrhythmia mechanisms in vitro and in animal models.
Research Applications of Ibutilide
In the research setting, ibutilide is primarily employed as a pharmacological probe to investigate cardiac ion channel function, particularly the hERG/IKr channel. Key research applications include:
- Atrial fibrillation (AF) and atrial flutter models: Ibutilide is used to pharmacologically cardiovert or maintain arrhythmia in isolated heart preparations and animal models, enabling mechanistic studies of AF and flutter.
- Action potential duration studies: Researchers use ibutilide to selectively prolong APD in cardiomyocyte preparations, helping dissect the contribution of individual ion currents to overall repolarization.
- hERG channel pharmacology: As a reference IKr blocker, ibutilide serves as a positive control in patch-clamp electrophysiology assays and cardiotoxicity screening studies.
- Drug interaction studies: Ibutilide is used to model QT-prolonging drug effects, supporting safety pharmacology and drug-drug interaction research.
Handling, Solubility, and Storage Guidelines
Solubility: Ibutilide is soluble in organic solvents such as DMSO and ethanol. Aqueous solubility at physiological pH is limited; if aqueous solutions are required, prepare stock solutions in DMSO or ethanol and dilute into the aqueous buffer immediately before use, keeping the final organic solvent concentration below levels that could affect the biological assay (typically ≤0.1% DMSO).
Preparation of stock solutions: Prepare concentrated stock solutions in DMSO (recommended) and store in single-use aliquots at -20 °C to avoid repeated freeze-thaw cycles, which can degrade compound integrity.
Storage: Store the solid compound at -20 °C in a tightly sealed container, protected from light and moisture. Under these conditions, the reagent is expected to remain stable for an extended period; consult the Certificate of Analysis (CoA) for the specific expiry date.
Safety: Handle ibutilide with standard laboratory precautions. Wear appropriate PPE including gloves, eye protection, and a lab coat. Consult the Safety Data Sheet (SDS) provided with your order for full hazard information and disposal guidance.
Ordering Ibutilide from Aladdin Scientific
Aladdin Scientific offers ibutilide (SKU: I610911) as a research-grade reagent. When placing your order, please verify the following to ensure you receive the correct product and documentation:
- Purity and specification: Check the product listing and Certificate of Analysis for purity grade, batch-specific analytical data, and any characterization data relevant to your assay requirements.
- Quantity: Ibutilide is available in research quantities; contact our technical sales team if you require custom pack sizes or bulk quantities.
- Documentation: A CoA and SDS are available for download from the product page or upon request. These documents are essential for compliance, quality management, and safe handling.
- Shipping and storage on receipt: Upon receipt, transfer the compound to -20 °C storage immediately. Inspect the packaging for damage and record the lot number for traceability.
For technical questions about ibutilide's suitability for your specific assay, contact Aladdin Scientific's technical support team.
Frequently asked questions
What is the primary mechanism of action of ibutilide?
Ibutilide prolongs cardiac action potential duration primarily by blocking the rapid delayed rectifier potassium channel (IKr/hERG) and by activating a slow inward sodium current. These combined effects delay cardiac repolarization and extend the effective refractory period in atrial and ventricular tissue.
What solvents can be used to dissolve ibutilide for in vitro experiments?
Ibutilide is soluble in DMSO and ethanol, both of which are suitable for preparing stock solutions for in vitro research use. When using DMSO, ensure that the final concentration in the biological assay does not exceed 0.1% to minimize solvent-related effects on cell viability or ion channel activity. Aqueous solubility is limited at physiological pH, so direct dissolution in buffer is not recommended without prior organic solvent stock preparation.
How should ibutilide reagent be stored to maintain stability?
The solid form of ibutilide should be stored at -20 °C in a tightly sealed container, protected from light and moisture. Stock solutions in DMSO should be aliquoted and stored at -20 °C to avoid repeated freeze-thaw cycles. Always refer to the Certificate of Analysis provided with your specific lot for confirmed expiry and stability information.
Is ibutilide suitable as a positive control in hERG channel assays?
Yes, ibutilide is widely used as a reference IKr blocker and is appropriate as a positive control in patch-clamp electrophysiology studies and fluorescence-based hERG channel assays. Its well-characterized pharmacology makes it useful for validating assay performance and benchmarking new test compounds in cardiotoxicity screening workflows.
What documentation is available when I order ibutilide (SKU: I610911) from Aladdin Scientific?
When ordering ibutilide (SKU: I610911) from Aladdin Scientific, you can access a batch-specific Certificate of Analysis (CoA) and a Safety Data Sheet (SDS). These documents are available for download from the product page or upon request from customer service, and they provide purity data, analytical characterization, hazard information, and disposal guidance.
References
- Lee KS. Ibutilide, a new compound with potent class III antiarrhythmic activity, activates a slow inward Na+ current in guinea pig ventricular cells. Journal of Pharmacology and Experimental Therapeutics. 1992.
- Naccarelli GV, et al. Ibutilide: a review of its pharmacology and clinical use. Expert Opinion on Pharmacotherapy. 2000.
- Sanguinetti MC, Jurkiewicz NK. Two components of cardiac delayed rectifier K+ current. Differential sensitivity to block by class III antiarrhythmic agents. Journal of General Physiology. 1990.
Products are supplied for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
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