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BCTC

N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide

A Potent Antagonist of TRPV1 and TRPM8 Channels

Cat #: B-110
Alternative Name N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 372.9
    Purity: >99% (HPLC)
    Effective concentration 1 nM – 100 nM.
    Structure
    Chemical name N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide.
    Molecular formula C20H25ClN4O.
    CAS No.: 393514-24-4
    PubChem CID 9929425
    Activity BCTC is a potent and selective antagonist of TRPV1 channels, shown to inhibit capsaicin-, pH- and PKC-induced responses of mouse TRPV1 with IC50 of 1.3, 0.59 and 0.37 nM, respectively.1,2 BCTC is also a blocker of TRPM8 channels, inhibiting rat TRPM8-mediated menthol and cold-evoked Ca2+ response with IC50 of 0.6 µM.3
    References-Activity
    1. Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
    2. Correll, C.C. et al. (2004) Neurosci. Lett. 370, 55.
    3. Madrid, R. et al. (2006) J. Neurosci. 26, 12512.
    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 1-10 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
    • Alomone Labs BCTC blocks TRPV1 channels expressed in C6 cells.
      Alomone Labs BCTC blocks TRPV1 channels expressed in C6 cells.
      Pre-incubation with 0.1 nM, 1 nM and 10 nM BCTC (#B-110), as indicated, inhibits the 1 µM capsaicin (#C-125)-evoked rise in intracellular Ca2+ (control). mTRPV1-C6 cells were loaded with Fluo-3-AM. Changes in intracellular Ca2+ were detected as changes in Fluo-3 fluorescent emission following agonist application.
    References - Scientific background
    1. Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
    2. McLeod, R.L. et al. (2006) Cough 2,10.
    3. Horton, J.S. et al. (2013) Channels (Austin) 7, 17.
    Scientific background

    BCTC (N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carbox-amide) is a potent, selective antagonist of the vanilloid receptor 1 (TRPV1) that is orally bioavailable. BCTC has the ability to block the activation of TRPV1 by capsaicin and by low pH. It has an IC50 of 35 nM3. Oral administration of BCTC in rats significantly reduces mechanical and thermal hyperalgesia associated with inflammation or nerve injury1.

    TRPV1 is a member of a distinct subgroup of the transient receptor potential (TRP) ion channel family, highly expressed in primary nociceptors. TRPV1 can be activated by several different stimuli such as heat, acid, certain arachidonic acid derivatives and direct phosphorylation via PKC. TRPV1 may serve a central role in inflammatory nociception2.

    Several recent studies have showed that administration of BCTC in patients suffering from symptoms of cardiac hypertrophy and heart failure can overcome loss-of-heart function.

    It has been suggested that TRPV1 blockade can be used as a new treatment strategy for cardiac hypertrophy and heart failure3.

    Target TRPV1 and TRPM8 channels
    Lyophilized Powder
    Last update: 02/01/2022

    BCTC (#B-110) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

    Applications

    Citations

    Citations
    Electrophysiology
    1. HEK 293 transfected cells.
      McArthur, J.R. et al. (2019) Br. J. Pharmacol. 176, 2264.

    Specifications

    Scientific Background

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