Pilsicainide hydrochloride

Non Antibodies

TTX-Sensitive NaV channels

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

308, 85

A Use-Dependent Anti-Arrhythmic NaV Channel Blocker

Centrifuge the vial before adding solvent (10, 000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.

41116134

Pilsicainide hydrochloride is an anti-arrhythmic drug1 and activity dependent Na+ (NaV) channel blocker2. Pilsicainide hydrochloride blocks human NaV1.4 channels with IC50s of 189 ± 10 µM at 0.1 Hz and 76 ± 7 µM at 10 Hz3.

Yes

Voltage-gated Na+ channels (VGSC, NaV) are critically important for electrogenesis and nerve impulse conduction. Certain Na+ channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of Nav in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation1.Pilsicainide is a class IC anti-arrhythmic drug widely used in the treatment of supraventricular and ventricular tachyarrhythmias in Japan2. Results from voltage clamp experiments show that Pilsicainide is a pure Na+ channel blocker with little or no effect on other cardiac channels, probably with the exception of HERG channels3-5.Measurements of Pilsicainide's ability to block hNaV1.4 channels resulted in half-maximum inhibitory concentrations (IC50) of 189 ± 10 µM at 0.1 Hz, and 76 ± 7 µM at 10 Hz. Effects of Pilsicainide were similar on skeletal muscle hNaV1.4, brain hNaV1.1 and heart hNaV1.5 channels.