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TC-I 2014

A Potent and Selective Blocker of TRPM8 Channels

Cat #: T-200
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 467.41
    Purity: >96%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name 3-[7-(Trifluoromethyl)-5-[2-(trifluoromethyl)phenyl]-1H-benzimidazol-2-yl]-1-oxa-2-azaspiro[4.5]dec-2-ene.
    Molecular formula C23H19F6N3O.
    CAS No.: 1221349-53-6
    Activity TC-I 2014 is a potent and selective TRPM8 blocker, inhibiting canine, rat, and human TRPM8-mediated Ca2+ influx with IC50 values of 0.8, 4.0, and 3.0 nM, respectively1.
    References-Activity
    1. Parks, D.J. et al. (2011) J. Med. Chem. 54, 233.
    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 +4°C.
    Solubility Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs TC-I 2014 inhibits TRPM8 channels expressed in HEK-293 cells.
      Alomone Labs TC-I 2014 inhibits TRPM8 channels expressed in HEK-293 cells.
      Dose response curve of TRPM8 inhibition by TC-I 2014 (#T-200), showing nearly complete inhibition at 1 µM. Cells were loaded with Calcium-5 dye, incubated for 10 min with increasing concentrations of TC-I 2014, and activated by 30 nM Icilin. Changes in intracellular Ca2+ following agonist application were detected as changes in 485 nm/525 nm fluorescence (RFU).
    References - Scientific background
    1. Parks, D.J. et al. (2011) J. Med. Chem. 54, 233.
    2. Behrendt, H.J. et al. (2004) Br. J. Pharmacol. 141, 737.
    Scientific background

    TC-I 2014 is a selective TRPM8 channel blocker. The compound shows high affinity towards TRPM8 and exhibits in vitro functional activity and good oral efficacy in an inflammatory model of neuropathic pain1. TC-I 2014 inhibits canine, rat, and human TRPM8 mediated Ca2+ influx functional assays with IC50 values of 0.8, 4.0, and 3.0 nM, respectively1.

    TRPM8 channel is a member of the TRP channels superfamily. TRPM8 is a Ca2+-permeable, nonselective cation channel that is activated by temperatures in the range of 8–28°C and by chemical agonists such as menthol and icilin. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons. Its expression is up-regulated in prostate cancer and other malignancies1,2.

    Target TRPM8 channel
    Last update: 06/11/2022

    TC-l-2014 (#T-200) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information