Free shipping starts now, no minimum, no coupons required!

Pilsicainide hydrochloride

SUN 1165

A Use-Dependent Anti-Arrhythmic NaV Channel Blocker

Cat #: P-145
Alternative Name SUN 1165
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 308.85
    Purity: >99%
    Effective concentration 10-200 µM.
    Structure
    Chemical name N-(2,6-Dimethylphenyl)tetrahydro-1H-pyrrolizine-7a(5H)-acetamide hydrochloride.
    Molecular formula C17H24N2O•HCl.
    CAS No.: 88069-49-2
    Activity 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.
    Shipping and storage 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.
    Solubility Water. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Pilsicainide hydrochloride inhibits NaV1.7 channels expressed in HEK293 cells.
      Alomone Labs Pilsicainide hydrochloride inhibits NaV1.7 channels expressed in HEK293 cells.
      A. Time course of current reversible inhibition by 100 μM Pilsicainide hydrochloride (#P-145). Currents were elicited by a voltage ramp from a holding potential of -100 mV to 60 mV (30 ms) delivered every 10 seconds. B. Example traces of current response to voltage ramp stimulation before and during 100 μM Pilsicainide hydrochloride application.
    References - Scientific background
    1. Amir, E. et al. (2006) J. Pain 7, S1.
    2. Hashimoto, Y. et al. (1993) Cardiovasc. Drug Rev. 11, 60.
    3. Hattori, Y. et al. (1992) Jpn. J. Pharmacol. 58, 365.
    4. Yamashita, T. et al. (1998) Jpn. Heart J. 39, 389.
    5. Wu, L. M. et al. (2003) J. Cardiovasc. Pharmacol. 42, 410.
    6. Desaphy, J. F. et al. (2010) Br. J. Pharmacol. 160, 1521.
    Scientific background

    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.

    Target TTX-Sensitive NaV channels
    Last update: 06/11/2022

    Pilsicainide hydrochloride (#P-145) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information