AMG 9810

A Blocker of TRPV1 Channels
    Cat #: A-180
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 337.4
    Purity: >96% (HPLC)
    Form Lyophilized powder.
    Effective concentration 0.5 nM - 50 µM.
    Structure
    • AMG 9810
    Chemical name (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide.
    Molecular formula C21H23NO3.
    CAS No.: 545395-94-6.
    Activity AMG 9810 blocks TRPV1 with IC50 ~0.01 µM1.
    References-Activity
    1. Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
    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 Ethanol 50 mM. Centrifuge all product preparations before use (10 000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • AMG 9810
      Alomone Labs AMG 9810 inhibits Olvanil-activated TRPV1 channels heterologously expressed in C-6 cells
      Cells were loaded with Fluo-3 AM and changes in intracellular Ca2+ was measured. Normalized fluorescence before (control, gray dotted line) and after application of 10 µM Olvanil (#O-115), either without or after incubation with 1 µM and 10 µM AMG 9810 (#A-180), black lines as indicated.
    References - Scientific background
    1. Gavva, N.R. et al. (2005) J. Pharmacol. Exp. Ther. 313, 474.
    Scientific background

    AMG 9810 (E)-3-(4-t-butylphenyl)-N-(2, 3- dihydrobenzo [b] [1,4] dioxin-6-yl) acrylamide is a potent, non-vanilloid, competitive antagonist of the vanilloid receptor 1 (TRPV1) with IC50 values for human TRPV1 of 24.5 nM and rat TRPV1 of 85.6 nM.

    Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands anandamide, N-arachidonoyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine.

    Furthermore, AMG 9810 blocks capsaicin-induced calcitonin gene-related peptide (CGRP) release and capsaicin-evoked depolarization in rat dorsal root ganglia neurons.

    Finally, AMG 9810 was shown to be a potent and selective antagonist of TRPV1 that can significantly reverse thermal and mechanical hyperalgesia in an animal model of inflammatory pain1.

    Target TRPV1 channels
    Image & Title AMG 9810
    Alomone Labs AMG 9810 inhibits TRPV1 endogenously expressed in mouse C2C12 myoblasts.Calcium influx in myoblast cells cultured with 0.9 mM CaCl2 at 37°C, exposed to 42°C, and then treated with AMG 9810 (#A-180). Calcium influx was increased by exposure to 42°C and decreased by treatment with AMG 9810.Adapted from Obi, S. et al. (2017) J. Appl. Physiol. 122, 683. with permission of The American Physiological Society.
    Last update: 24/01/2020

    AMG 9810 (#A-180) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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