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A KCNQ Channel Opener

Cat #: D-150
Alternative Name DMC
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 395.4
    Purity: >99%
    Effective concentration 10 µM.
    Chemical name 4-[5-(2,5-dimethylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide.
    Molecular formula C18H16F3N3O2S.
    CAS No.: 457639-26-8
    PubChem CID 11545682
    Activity 2,5-dimethylcelecoxib is a KCNQ channel opener in smooth muscle cells1.
    1. Brueggemann, L.I. et al. (2012) Am. J. Physiol. Lung Cell. Mol. Physiol. 302, L120.
    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 100 mM in 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 2,5-dimethylcelecoxib enhances KCNQ2/KCNQ3 heteromeric channels expressed in Xenopus oocytes.
      Alomone Labs 2,5-dimethylcelecoxib enhances KCNQ2/KCNQ3 heteromeric channels expressed in Xenopus oocytes.
      A. Time course of KCNQ2/KCNQ3 current enhancement by 10 and 100 µM 2,5-dimethylcelecoxib (#D-150) as measured at -40 mV. Currents were elicited by application of voltage ramp from a holding potential of -100 mV to 0 mV (800 msec). B. Superimposed example traces of current responses before and during perfusion of 10 and 100 µM 2,5-dimethylcelecoxib, as indicated (part of the response to ramp stimulation).
    References - Scientific background
    1. Schwake, M. et al. (2006) J. Neurosci. 26, 3757.
    2. Howard, R.J. et al. (2007) Neuron 53, 5.
    3. Brueggemann, L.I. et al. (2012) Am. J. Physiol. Lung Cell. Mol. Physiol. 302, L120.
    4. Jendrossek, V. (2013) Cancer Lett. 332, 2.
    Scientific background

    KV7 (KCNQ) channels 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 five different 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.

    2,5-Dimethylcelecoxib (DMC) is a synthetic opener of KCNQ channels in smooth muscle cells. It is a derivative of Celecoxib without its COX-2 inhibitory function. In asthma and other lung diseases, airways become hyperconstricted because of the secretion of various endogenous substances. DMC causes an increase in KCNQ currents and restores current amplitudes in guinea pig ASMC (air smooth muscle cells). This effect is also seen after the application of bronchoconstrictors such as methacholine and histamine, suggesting that DMC can regulate and dilate airway diameter in bronchoconstricting diseases3. DMC is a potent activator of apoptotic pathways and also suppresses production of prostaglandins in vitro by inhibiting cytokine-triggered upregulation of microsomal PGE-synthase-1. These properties may be valuable in the research of cancer4.

    Target KCNQ channels
    Last update: 06/11/2022

    2,5-dimethylcelecoxib (#D-150) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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