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Co 102862

V102862

A Potent, State-Dependent Blocker of Neuronal NaV Channels

Cat #: C-160
Alternative Name V102862
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 273.3
    Purity: >96% (HPLC)
    Effective concentration 0.1-200 μM
    Structure
    Chemical name 2-[[4-(4-Fluorophenoxy)phenyl]methylene]hydrazinecarboxamide.
    Molecular formula C14H12FN3O2.
    CAS No.: 181144-66-1
    Activity Co 102862 is a potent, broad spectrum and state-dependent blocker of neuronal voltage-gated Na+ channels that interacts selectively with inactivated states as opposed to resting states of the channel1. IC50 values are 0.28-15.9 µM in rat hippocampal neurons2. It is an anticonvulsant, demonstrating potent activity in rodent models of tonic/clonic and partial-complex seizures3.
    References-Activity
    1. Catterall, W.A. (1992) Physiol. Rev. 72, S15.
    2. Ilyin, V.I. et al. (2005) Br. J. Pharmacol. 144, 801.
    3. Carter, R.B. et al. (1997) Soc. Neurosci. Absrt. 23, 2163.
    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 Co 102862 inhibits NaV1.7 channel currents in HEK293 cells.
      Alomone Labs Co 102862 inhibits NaV1.7 channel currents in HEK293 cells.
      A. Time course of current reversible inhibition by 50 µM Co 102862 (#C-160). 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 application of 50 µM Co 102862.
    References - Scientific background
    1. Catterall, W.A. (1992) Physiol. Rev. 72, S15.
    2. Catterall, W.A. (2000) Neuron 26, 13.
    3. Bean, B.P. et al. (1983) J. Gen. Physiol. 81, 613.
    4. Hondeghem, L.M. and Katzung, B.G. (1984) Annu. Rev. Pharmacol. Toxicol. 24, 387.
    5. Butterworth, J.F. 4th and Strichartz, G.R. (1990) Anesthesiology 72, 711.
    6. Kuo, C.C. and Bean, B.P. (1994) Mol. Pharmacol. 46, 716.
    7. Xie, X.M. et al. (1995) Pfluegers Arch. Eur. J. Physiol. 430, 437.
    8. Kuo, C.C. et al. (1997) Mol. Pharmacol. 51, 1077.
    9. Kuo, C.C. et al. (2000) Mol. Pharmacol. 57, 135.
    10. Yang, Y.C. and Kuo, C.C. (2002) Mol. Pharmacol. 62, 1228.
    11. Ilyin, V.I. et al. (2005) Br. J. Pharmacol. 144, 801.
    12. Carter, R.B. et al. (1997) Soc. Neurosci. Absrt. 23, 2163.
    Scientific background

    Voltage-gated Na+ channels play key roles in determining neuronal excitability1,2. Voltage- and use-dependent blockage of voltage-gated Na+ channels appear to be important in the mechanism of action of many anticonvulsants (e.g. phenytoin (PHT), carbamazepine (CBZ) and lamotrigine (LTG)), local anesthetics (e.g. lidocaine and bupivacaine) and Class I antiarrhythmics3-10.

    Co 102862 is a potent, broad spectrum and state-dependent blocker of neuronal voltage-gated Na+ channels that interacts selectively with inactivated states as opposed to resting states of the channel11. IC50 values are 0.28-15.9 μM in rat hippocampal neurons11.

    Co 102862 is an anticonvulsant, demonstrating potent activity in rodent models of tonic/clonic and partial-complex seizures12.

    Target NaV Na+ channels
    Last update: 08/06/2021

    Co 102862 (#C-160) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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