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Ralfinamide mesylate


A Use-Dependent Blocker of NaV Channels

Cat #: R-105
Alternative Name NW-1029®
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 398.5
    Purity: >99%
    Effective concentration 10-200 µM.
    Chemical name (2S)-2-[[[4-[(2-Fluorophenyl) methoxy]phenyl]methyl]amino]-propanamide methanesulfonate.
    Molecular formula C18H23FN2O5S●CH3SO3H.
    CAS No.: 202825-45-4
    Activity Ralfinamide mesylate is a Na+ channel blocker1. Its IC50 values for tonic block of half-maximal inactivated tetrodotoxin (TTX)-resistant and TTX-sensitive currents are 10 and 22 μM, respectively1. Ralfinamide displays analgesic effects in animal models of inflammatory and neuropathic pain2.
    1. Stummann, T.C. et al.  (2005) Eur. J. Pharmacol. 510197.
    2. Veneroni, O. et al. (2003) Pain. 102, 17.
    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.
    Our bioassay
    • Alomone Labs Ralfinamide mesylate inhibits NaV1.7 channels expressed in HEK293 cells.
      Alomone Labs Ralfinamide mesylate inhibits NaV1.7 channels expressed in HEK293 cells.
      A: Time course of current reversible inhibition by 100 μM Ralfinamide mesylate (#R-105). 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 Ralfinamide mesylate application.
    References - Scientific background
    1. Zimmermann, M. et al. (2001) Eur. J. Phamacol. 429, 23.
    2. Goldin, A. L. et al. (2001) Annu. Rev. Physiol 63, 871.
    3. Stummann, T. C. et al. (2005) Eur. J. Pharmacol. 510, 197.
    4. Veneroni, O. et al. (2003) Pain. 102, 17.
    5. Zhang, S. H. et al. (2008) Pain 139, 293.
    6. Yamane, H. et al. (2007) Exp. Neurol. 208, 63.
    Scientific background

    Voltage-gated Na+ channels (VGSCs) comprise a large multi-gene family encoding individual subtypes that can be differentiated on the basis of primary structure, biophysical properties and sensitivity to the neurotoxin tetrodotoxin1-2. Most VGSCs, termed TTX-sensitive (TTXs), have been both found in brain and sensory neurons where they have a low threshold for activation and rapid inactivation kinetics; by contrast other VGSCs are termed TTX-resistant (TTXr). These may play a key role in persistent pain states, including neuropathic and chronic inflammatory pain.

    Ralfinamide mesylate (NW-1029) is a Na+ channel blocker that suppresses tetrodotoxin (TTX)-resistant Na+ currents in small to medium size (C-type) dorsal root ganglia (DRG) neurons about twice as selectively as it blocks TTX-sensitive currents in the same neurons; IC50 values for tonic block of half-maximal inactivated tetrodotoxin-resistant and tetrodotoxin-sensitive currents are 10 μM and 22 μM, respectively3. The blocking action of ralfinamide shows frequency and voltage dependence3. In experimental animal models of inflammatory and neuropathic pain, systemic administration of ralfinamide elicits anti-nociceptive effects4-6.

    Target NaV Na+ channels
    Last update: 24/01/2021

    Ralfinamide mesylate (#R-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background


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