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A Blocker of CaV1 Channels, a COX-2 Inhibitor and an Opener of KCNQ Channels 

Cat #: C-190
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 381.4
    Purity: >98.5%
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
    Chemical name 4-[5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-benzenesulfonamide.
    Molecular formula C17H14F3N3O2S.
    CAS No.: 169590-42-5
    Activity Celecoxib is an L-type Ca2+ channel blocker and an opener of KCNQ channels1.
    1. Zhang, Y. et al. (2007) Pharmacol. Res. 56, 267.
    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 for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Celecoxib blocks L-type CaV channel currents expressed in Xenopus oocytes.
      Alomone Labs Celecoxib blocks L-type CaV channel currents expressed in Xenopus oocytes.
      A. Time course of CaV1.2 (co-expressed with α2δ1 and β1 auxiliary subunits) currents, elicited by 100 ms voltage ramp from holding potential of -100 mV to +50 mV, delivered every 10 seconds. Application of 100 µM Celecoxib (#C-190) inhibits the current amplitude (period of application indicated by horizontal bar). B. Representative current traces before and during application of 100 µM Celecoxib as indicated.
    References - Scientific background
    1. Mccormack, P.L. (2011) Drugs 71, 2457.
    2. Brueggemann, L.I. et al. (2009) Mol. Pharmacol. 76, 1053.
    3. Macias, A. et al. (2010) J. Mol. Cell. Cardiol. 49, 984.
    4. Zweers, M.C. et al. (2011) Arthritis Res. Ther. 13, 239.
    5. Jendrossek, V. (2013) Cancer Lett. 332, 313.
    Scientific background

    Celecoxib is a non-steroidal anti-inflammatory drug (NSAID), which selectively inhibits the enzyme cyclo-oxygenase (COX)-2. NSAIDs are widely used to treat pain caused by inflammation-related complications, which are symptomatic in chronic or acute pathologies. Allegedly, NSAIDs prevent pain by inhibiting COX-1 and COX-2, which help to synthesize mediators of pain such as prostaglandins. While COX-1 is normally present in most healthy tissues, COX-2 is expressed only in damaged tissues and is mainly induced by inflammatory factors1.

    The first generation of NSAIDs targeted both COXs. This led to unwanted gastrointestinal side effects due to the inhibition of COX-1. To minimize intervention with COX-1, selective COX-2 inhibitors (coxibs) were then developed. Celecoxib was the first clinically proven coxib. In vitro assays have shown that celecoxib inhibits COX-2 with an IC50 of 15 μmol/L. In addition, it efficiently blocks L-type Ca2+ channels (CaV1), but enhances the K+ voltage-gated channel KCNQ activity2,3.

    Clinical trials have shown that celecoxib is a useful therapy for symptomatic pain relief, usually in various joint-related diseases such as osteoarthritis, rheumatoid arthritis, and Ankylosing Spondylitis. Unfortunately, it increases the risk of cardiovascular diseases, probably due to interfering with cardiac K+ channels1.

    It was suggested that the drug might be implicated in other aspects of the COX-2 signaling pathway than the anti-inflammation effects4. Celecoxib is also being evaluated as a potential anti-cancer drug as it was found to induce apoptosis via specific pathways independent of COX-25.

    Target L-type Ca2+ and KCNQ channels
    Last update: 25/07/2021

    Celecoxib (#C-190) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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