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Chembridge-5861528

TCS 5861528, ST50720185

A Selective Blocker of TRPA1 Channel

Cat #: C-235
Alternative Name TCS 5861528, ST50720185
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 369.4
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name N-(4-butan-2-ylphenyl)-2-(1,3-dimethyl-2,6-dioxopurin-7-yl)acetamide.
    Molecular formula C19H23N5O3.
    CAS No.: 332117-28-9
    PubChem CID 2873523
    Activity Chembridge-5861528 blocks TRPA1 channels and has an IC50 of 0.3 µM in rat-TRPA1 transfected HEK 293 cells1.
    References-Activity
    1. Wei, H. et al. (2010) Neuropharmacology 58, 578.
    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 Up 100 mM in DMSO. Centrifuge all product preparations before use (5,000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Chembridge-5861528 inhibits Allyl isothiocyanate induced calcium signal in TRPA1 expressing cells. 
      Alomone Labs Chembridge-5861528 inhibits Allyl isothiocyanate induced calcium signal in TRPA1 expressing cells
      Dose-response curve for the inhibition of human TRPA1 expressing HEK-293 cells loaded with Calcium 5 dye for changes in intracellular Ca2+ measurements. Allyl isothiocyanate (100 µM)-induced calcium signal was inhibited by 5 µM Chembridge-5861528 (#C-235), with estimated IC50 of about 4 µM.
    References - Scientific background
    1. Wei, H. et al. (2010) Neuropharmacology 58, 578.
    2. Benemei, S. et al. (2013) J. Headache Pain 14, 71.
    Scientific background

    Chembridge-5861528 (CHEM), a derivative of HC-030031 compound, is a potent and selective TRPA1 (TRP ankyrin 1) channel antagonist. TRPA1 channels play an important role in models of inflammatory and neuropathic pain and have the ability to detect pungent or irritant compounds.

    Administration of Chembridge-5861528 attenuates diabetic hypersensitivity. It reduces hypersensitivity by suppressing the TRPA1 channel-mediated facilitation of transmitter release from central terminals of primary afferent nerve fibers1,2.

    Blocking TRPA1 channels may help in migraine attack and can be used as a possible target for its treatment.

    Evidence in several studies shows that TRPA1 antagonists could serve as novel therapeutic strategies for the treatment of chemotherapeutic-induced peripheral neuropathy2.

    Target TRPA1 channels
    Last update: 25/04/2021

    Chembridge-5861528 (#C-235) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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