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A 784168

CHEMBL482834

A Potent Blocker of TRPV1 Channel

Cat #: A-345
Alternative Name CHEMBL482834
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 479.4
    Purity: >99%
    Effective concentration 10 nM - 1 µM.
    Structure
    Chemical name 1-[3-(trifluoromethyl)pyridin-2-yl]-N-[4-(trifluoromethylsulfonyl)phenyl]-3,6-dihydro-2H-pyridine-4-carboxamide.
    Molecular formula C19H15F6N3O3S.
    CAS No.: 824982-41-4
    PubChem CID 11420211
    Activity A 784168 is a potent TRPV1 antagonist, inhibiting human TRPV1 activation by 50 nM capsaicin with IC50 of 25 nM1.
    References-Activity
    1. Cui, M. et al. (2006) J. Neurosci. 26, 9385.
    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 100 mM in DMSO or 50 mM in ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs A 784168 inhibits TRPV1 channels expressed in C6 cells. 
      Alomone Labs A 784168 inhibits TRPV1 channels expressed in C6 cells. 
      mTRPV1-C6 cells were loaded with Fluo-3 AM. Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following agonist application. 10 minutes pre-incubation with 0.1 µM and 1 µM A 784168 (#A-345) inhibited 1 µM capsaicin-evoked rise in intracellular Ca2+. Normalized fluorescence before and after application (arrow) of 1 µM capsaicin in cells pre-incubated with DMSO-equivalent control, 0.1 µM and 1 µM A 784168 (as indicated).
    References - Scientific background
    1. Cui, M. et al. (2006) J. Neurosci. 26, 9385.
    Scientific background

    A 784168 is a synthetic and potent antagonist of the TRPV1 channel. A 784168 inhibits human TRPV1 activation by 50 nM capsaicin with an IC50 of 25 nM. A 784168 was found to produce inhibition in 1321N1 astrocytoma cells expressing recombinant human TRPV1 and also in HEK 293 cells. In addition to its inhibition of TRPV1, A 784168 was found to be a very weak antagonist of TRPM8 (IC50 = 20.8 µM) with no effect on TRPA1 channels and a variety of receptors including adenosine, angiotensin, α- and β-adrenergic receptors. A 784168 has a plasma binding capacity of 93.5±0.9% and oral bioavailability of 33%. A 784168 volume of distribution is 12.4L/kg and it has high blood-brain barrier penetrance. Administration of oral A 784168 reduces acute nociceptive behavior induced by capsaicin injection and chronic thermal hyperalgesia induced by CFA injection in a rat model1.

    Target TRPV1 channel
    Lyophilized Powder
    Last update: 12/08/2021

    A 784168 (#A-345) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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