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AMG2850

A Potent and Selective Blocker of TRPM8 Channels

Cat #: A-340
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 417.35
    Purity: >99% (HPLC)
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name ((R)-8-(4-(trifluoromethyl)phenyl)-N-((S)-1,1,1-trifluoropropan-2-yl)-5,6-dihydro-1,7-naphthyridine-7(8H)-carboxamide).
    Molecular formula C19H17F6N3O.
    CAS No.: 1470018-52-0
    Activity AMG2850 is a potent and selective blocker of TRPM8 channels. It was shown in vitro to inhibit rat TRPM8 cold, menthol and icilin activation with IC50 of 7.3 nM, 156 nM and 204 nM, respectively. Highly selective for TRPM8 over TRPV1 and TRPA1 channels and orally bioavailable (Fpo>40%)1,2.
    References-Activity
    1. Gavva, N.R. et al. (2012) Mol. Pain 8, 36.
    2. Lehto, S.G. et al. (2015) Naunyn Schmiedebergs Arch. Pharmacol. 388, 465.
    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 200 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 AMG2850 blocks TRPM8 channels expressed in HEK 293 cells.
      Alomone Labs AMG2850 blocks TRPM8 channels expressed in HEK 293 cells.
      Dose-response curve of TRPM8 inhibition by AMG2850 (#A-340), showing full inhibition at 2 µM (IC50 = 346 nM). Cells were loaded with Calcium-5 dye, incubated for 10 min with increasing concentrations of AMG2850, 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. Gavva, N.R. et al. (2012) Mol. Pain 8, 36.
    2. Lehto, S.G. et al. (2015) Naunyn Schmiedebergs Arch. Pharmacol. 388, 465.
    3. Behrendt, H.J. et al. (2004) Br. J. Pharmacol. 141, 737.
    4. Tsumura, M. et al. (2013) PLoS One 8, e82233.
    Scientific background

    AMG2850 is a selective blocker of TRPM8 channels. The compound shows high selectivity towards TRPM8 over TRPV1 and TRPA1 channels. AMG2850 potently inhibits the menthol and cold-induced increase in intracellular Ca2+ in cells expressing rat TRPM8. In vitro, it was shown to inhibit rat TRPM8 against cold, menthol and icilin activation with IC50 of 7.3 nM, 156 nM and 204 nM, respectively1,2. AMG2850 is orally bioavailable and its plasma half-life (T1/2) in rats is 3.5 hours1,2.

    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 neurons3,4.

    Target TRPM8 channel
    Last update: 11/04/2021

    AMG2850 (#A-340) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

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    Scientific Background

    Citations

    Citations
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