AG 3-5
A Potent Activator of TRPM8 Channels
    Cat #: I-145
    Alternative Name AG 3-5
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 311.29
    Purity: >95%
    Effective concentration 1 nM – 1 µM.
      • Icilin
    Chemical name 3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-1,4-dihydropyrimidin-2-one.
    Molecular formula C16H13N3O4.
    CAS No.: 36945-98-9.
    PubChem CID 161930
    Activity Icilin is a potent TRPM8 channel activator (EC50 = 0.2 µM)1.
    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 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.
      • Icilin
        Alomone Labs Icilin activates TRPM8 channels expressed in HEK-293 cells.
        Dose response curve of human TRPM8 activation by increasing concentrations of Icilin (#I-145). EC50 was determined at 27 nM. hTRPM8/HEK-293 cells were loaded with Calcium-5 dye. Increase in intracellular Ca2+ levels following Icilin application was detected as a rise in 485 nm/525 nm fluorescence (RFU).
    References - Scientific background
    • 1. Behrendt, H.J. et al. (2004) Br. J. Pharmacol. 141, 737.
    • 2. Kayano, T. et al. (2010) J. Vet. Med. Sci. 72, 1531.
    • 3. Kim, J. et al. (2011) Brain Res. 1384, 110.
    • 4. Tsumura, Met al. (2013) PLoS One  8, e82233.
      • Icilin is a synthetic cooling substance that acts as a potent TRPM8 channel activator with an EC50 value of 0.2 ± 0.1μM1. This compound also shown to activate TRPA1 ion channel but at higher concentrations. Activation of TRPM8 channel by icilin produces Na+ and Ca2+ ion influx that results in cellular depolarization and the feeling of cold. Icilin has the ability to produce behavioral activation in rats and mice1-3.

        TRPM8 is a Ca2+-permeable channel, a member of the ‘long' or melastatin (M) group of TRP channels and is activated by temperatures in the range of 8-28°C or by cooling compounds such as icilin. The TRPM8 gene is expressed and up-regulated in prostate cancer and other malignancies. TRPM8 channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons1,4.

    Target TRPM8 channel
    Last update: 13/11/2019

    Icilin (#I-145) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use