Ranolazine

Ranexa, (-)-Ranolazine, Latixa, CVT-303, Ran4
A Blocker of Voltage-Gated Na+ Channels
Cat #: R-110
Alternative Name Ranexa, (-)-Ranolazine, Latixa, CVT-303, Ran4
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 427
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 1 µM - 1 mM.
    Chemical name (RS)-N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)-propyl]piperazin-1-yl]acetamide.
    Molecular formula C24H33N3O4.
    CAS No.: 95635-55-5, 142387-99-3.
    Activity NaV inhibitor with IC50 of about 50 µM1.
      • Wang, G.K. et al. (2008) Mol. Pharmacol. 73, 940.

    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 DMSO. 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.
      • Alomone Labs Ranolazine inhibits NaV1.5 channels heterologously expressed in HEK-293 cells.
        A. Time course of the cardiac NaV1.5 (expressed in HEK-293 cells) current inhibition by 200 and 500 µM Ranolazine (#R-110). Currents were elicited by application of voltage ramps from a holding potential of -100 mV to 0 mV (50 msec). B. Superimposed example traces of current responses before and during perfusion of 200 and 500 µM Ranolazine as indicated.
        Alomone Labs Ranolazine inhibits NaV1.4 channels heterologously expressed in Xenopus oocytes cells.
        A. Time course of the skeletal NaV1.4 current inhibition by 100, 200 and 500 µM Ranolazine (#R-110). Currents were elicited by application of voltage ramps from a holding potential of -100 mV to +30 mV (100 msec). B. Superimposed example traces of current responses before and during perfusion of 100, 200 and 500 µM Ranolazine as indicated.
      • Voltage-gated Na+ (NaV) channels are essential for the generation and propagation of action potentials in excitable membranes. The NaV channel protein contains four homologous domains (D1-D4), each with six transmembrane segments (S1-S6). There are 9 isoforms (NaV1.1-1.9) found among mammalian excitable tissues, including central nervous system, peripheral nervous system, skeletal muscle, and heart1.

        Ranolazine is an antianginal and anti-ischemic drug that is used in patients with chronic angina2. Ranolazine displays a broad pharmacological profile on a number of targets and has complex electrophysiological effects in myocardium3. This drug seems to preferentially reduce the persistent late cardiac NaV1.5 Na+ currents with a 50% inhibitory concentration (IC50) of 15 μM, whereas normal transient Na+ currents are less affected, with an IC50 of 135 μM4. The binding site of ranolazine in human cardiac Na+ channels is probably the same as the local anesthetic (LA) receptor within the inner cavity of the Na+ channel, because a single mutation in this channel (e.g. residue hNaV1.5-F1760A) alters the ranolazine binding affinity drastically4.

    Target NaV Na+ channels
    Last update: 12/03/2019

    Ranolazine (#R-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use