A-889425

A Blocker of TRPV1 Channels
Cat #: A-195
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 425.4
    Purity: >98% (HPLC)
    Form Lyophilized powder.
    Effective concentration 0.5 nM - 50 µM.
    Chemical name 1-(3-methylpyridin-2-yl)-N-(4-(trifluoromethylsulfonyl)phenyl)-1,2,3,6-tetrahydropyridine-4-carboxamide.
    Molecular formula C19H18F3N3O3S.
    CAS No.: 1072921-02-8.
    Activity A-889425 blocks TRPV1 channels with an IC50 of 335 nM (rat) and 34 nM (human)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 DMSO up to 100 mM. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • Alomone Labs A-889425 inhibits capsaicin activated TRPV1 channels heterologously expressed in C-6 cells.
        Cells were loaded with Fluo-3 AM and changes in intracellular Ca2+ were measured. Normalized fluorescence before (control, gray dotted line) and after application of 1µM Capsaicin (#C-125), (black lines) in cells pre-incubated without or with 0.5 µM A-889425 (#A-195), (top and bottom lines, as indicated). 10 min pre-incubation with 0.5 µM A-889425 abolishes capsaicin-evoked rise in intracellular Ca2+.
      • TRPV1 (transient receptor potential vanilloid family type 1) channels are activated and/or modulated by noxious heat, capsaicin, protons and other endogenous agents released following tissue injury.

        A-889425 is a selective and competitive TRPV1 channel blocker with an IC50 of 335 nM to displace capsaicin at rat receptors, and has good penetration into the CNS1. In the somatic sensory system, receptor-selective TRPV1 antagonists, such as A-889425 attenuate mechanical hyperalgesia in models of inflammatory, osteoarthritic, and neuropathic pain2. Administration of A-889425 inhibited mechanically evoked activity of wide dynamic range (WDR) neurons in the rat spinal dorsal horn under conditions of peripheral inflammation but not in uninjured rats1. In addition to actions on the nociceptive system, several TRPV1 blockers like A-889425 have been reported to also affect thermoregulation by transiently raising core body temperature following systemic administration in both animals and humans3.

    Target TRPV1 channels
    Last update: 28/05/2019

    A-889425 (#A-195) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use