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AG 3-5

A Potent Activator of TRPM8 Channels

Cat #: I-145
Alternative Name AG 3-5
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 311.29
    Purity: >95%
    Effective concentration 1 nM – 1 µM.
    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.
    1. Behrendt, H.J. et al. (2004) Br. J. Pharmacol. 141, 737.
    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.
    Our bioassay
    • Alomone Labs Icilin activates TRPM8 channels expressed in HEK-293 cells.
      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.
    Scientific background

    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: 06/11/2022

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

    For research purposes only, not for human use



    Scientific Background

    Shipping and Ordering information