SB-366791

A Specific and Potent TRPV1 Blocker
    Cat #: S-180
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 287.7
    Purity: >99%
    Effective concentration 5 nM - 50 µM.
    Structure
    • SB-366791
    Chemical name (E)-3-(4-chlorophenyl)-N-(3-methoxyphenyl)prop-2-enamide.
    Molecular formula C16H14ClNO2.
    CAS No.: 472981-92-3.
    PubChem CID 667594
    Activity SB-366791 is a TRPV1 channel antagonist1.
    References-Activity
    1. Gunthorpe, M.J. et al. (2004) Neuropharmacology 46, 133.
    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
    • SB-366791
      Alomone Labs SB-366791 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 5 and 50 µM SB-366791 (#S-180) 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 with 0 nM (DMSO equivalent control, black), 5 µM (gray) or 50 µM SB-366791 (dotted line).
    References - Scientific background
    1. Gunthorpe, M.J. et al. (2004) Neuropharmacology 46, 133.
    2. Niiyama, Y. et al. (2009) Br. J. Anaesth. 102, 251.
    3. McLeod, R.L. et al. (2006) Cough 2, 10.
    4. Uchytilova, E. et al. (2014) Mol. Pain 10, 67.
    Scientific background

    SB-366791 is a potent and selective TRPV1 channel antagonist1. Novel strategies for the treatment of bone cancer pain have shown that morphine in combination with SB-366791 has potent analgesic effects on bone cancer pain2.

    TRPV1 (Vanilloid receptor-1) is a member of a distinct subgroup of transient receptor potential (TRP) family. These channels are highly expressed on 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 nociception3.

    Studies have shown that local intradermal treatment with SB-366791 compound has the ability to reduce thermal hyperalgesia and mechanical allodynia without affecting mechanical hyperalgesia4.

    Target TRPV1 channels
    Last update: 24/01/2020

    SB-366791 (#S-180) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information