Capsazepine

A Selective TRPV1 Blocker and an Activator of ENaCγ Channels
    Cat #: C-120
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 376.9
    Purity: >97%
    Effective concentration 0.1-100 µM.
    Structure
    • Capsazepine
    Chemical name N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide.
    Molecular formula C19H21ClN2O2S.
    CAS No.: 138977-28-3.
    PubChem CID 2733484
    Activity Capsazepine is a selective antagonist of the vanilloid VR1 receptor (TRPV1) with IC50 of 40 nM, and an activator of the ENaC channels.
    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 100 mM in DMSO. 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
    • Capsazepine
      Alomone Labs Capsazepine inhibits TRPV1 channels expressed in C6 cells.
      mTRPV1-C6 cells were loaded with Fluo-3AM. Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following agonist application. 5 minutes pre-incubation with 10 µM Capsazepine (#C-120) inhibited 10 µM Capsaicin (#C-125)-evoked rise in intracellular Ca2+. Normalized fluorescence before and after application (arrow) of 10 µM Capsaicin in cells pre-incubated without (black) or with 10 µM Capsazepine (gray).
    References - Scientific background
    1. Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
    2. Shukla, A. et al. (2014) PLoS One 9, e100797.
    3. Mahmmoud, Y.A. et al. (2014) PLoS One 9, e96909.
    4. Gonzalez-Reyes, L.E. et al. (2013) Exp. Neurol. 250, 321.
    5. Yamamura, H. et al. (2004) J. Biol. Chem. 279, 44483.
    6. McLeod, R.L. et al. (2006) Cough 2, 10.
    Scientific background

    Capsazepine is a synthetic, competitive and selective antagonist of TRPV1 (transient receptor potential vanilloid 1)1 and an activator of amiloride-sensitive epithelial Na+ channel gamma (ENaCγ). It also inhibits K+-dependent ATP hydrolysis with no effect on Na+-ATPase2,3.

    Capsazepine is being used in in vitro and in vivo pharmacological studies as a standard TRPV1 competitive antagonist.

    Capsazepine exhibits potent inhibition of expression of the iNOS gene in LPS-stimulated murine macrophages through inactivation of NF-κB4.

    The amiloride-sensitive epithelial Na+ channel (ENaC) regulates Na+ homeostasis into cells and across epithelia5.

    TRPV1 is a member of a distinct subgroup of transient receptor potential (TRP) ion channels. These channels are highly expressed on primary nociceptors and can be activated by several different stimuli such as heat, acid, certain arachidonic acid derivatives and direct phosphorylation via PKC6.

    Target TRPV1, ENaCγ channels
    Last update: 24/01/2020

    Capsazepine (#C-120) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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