Diclofenac sodium salt

Sodium diclofenac, Anthraxiton, Batafil, Delimon
An Opener of KCNQ Channels
    Cat #: D-181
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 318.1
    Purity: >99%
    Effective concentration 1 µM-500 µM.
    Structure
    Chemical name sodium;2-[2-(2,6-dichloroanilino)phenyl]acetate.
    Molecular formula C14H10Cl2NNaO2.
    CAS No.: 15307-79-6.
    Activity Diclofenac is a KCNQ opener with anti-nociceptive properties1.
    References - Activity
    1. Peretz, A. et al. (2005) Mol. Pharmacol. 67, 1053.

    Storage before reconstitution 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.
    Reconstitution 50 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage after reconstitution Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    Alomone Labs Diclofenac sodium salt enhances KCNQ2/KCNQ3 heteromeric channels expressed in Xenopus oocytes. 
    A. Time course of KCNQ2/KCNQ3 current enhancement by 100, 200 and 500 µM Diclofenac sodium salt (#D-181). Currents were elicited by application of voltage step from a holding potential of -100 mV to -60 mV (800 msec). B. Superimposed example traces of current responses before and during perfusion of 100, 200 and 500 µM Diclofenac sodium salt, as indicated.
    References - Scientific Background
    1. Schwake, M. et al. (2006) J. Neurosci. 26, 3757.
    2. Howard, R.J. et al. (2007) Neuron 53, 663.
    3. Peretz, A. et al. (2005) Mol. Pharmacol. 67, 1053.
    Scientific background

    KV7 or KCNQs are voltage-gated potassium channels. These channels are mainly responsible for the cardiac and auditory IKs current and the neuronal M-current but can be found in other tissues as well. Voltage-gated potassium channels are tetramers of α-subunits, which surround a K+-selective pore1. The different five KCNQ subtypes have distinct assembly preferences encoded by a C-terminal cytoplasmic assembly domain, the A-domain Tail. This domain is a self-assembling, parallel, four-stranded coiled coil2.

    Diclofenac (Voltaren) is a synthetic opener of KCNQ channels with an effective concentration of 1-500 μM. The opening mechanism by Diclofenac is not fully understood and it is hypothesized that this is achieved by either destabilizing the closed channel conformation or stabilizing the channel in its open state. Diclofenac reduces evoked and spontaneous action potentials in neuronal cells. In addition, it also enhances M-currents and to exhibit anti-convulsing properties thus making it a possible drug template for the treatment of neuronal hyper excitability pathologies such as epilepsy, migraine or neuropathic pain. Diclofenac is also a non-steroidal anti-inflammatory drug preventing inflammation via the non-selective inhibition of the enzymes COX1 and COX2 and the reduction of Prostaglandin production3.

    Target KCNQ channels
    Last update: 07/01/2019

    Diclofenac sodium salt (#D-181) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use