BQ-123 sodium salt

Cyclo(D-trp-D-asp-L-pro-D-val-L-leu) sodium
A Selective Antagonist of Endothelin A Receptors
    Cat #: B-185
    Alternative Name Cyclo(D-trp-D-asp-L-pro-D-val-L-leu) sodium
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 632.69
    Purity: >98%
    Effective concentration 10 nM – 10 µM.
    Sequence Cyclo (D-trp-D-asp-L-pro-D-val-L-leu).
    Modifications Supplied as sodium salt.
      • BQ-123 sodium salt
    Chemical name 2-[(3R,6R,9S,12R,15S)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl] acetate sodium.
    Molecular formula C31H41N6NaO7.
    CAS No.: 136655-57-7.
    PubChem CID 443289
    Activity BQ-123, a cyclic peptide provided as a sodium salt, is a potent and selective antagonist of ET-A endothelin receptors, exhibiting a 1000-fold selectivity for ET-A over ET-B receptors (inhibiting endothelin-1 radioligand binding to ET-A and ET-B with IC50 of 22 nM and 18 µM, respectively). In vitro, BQ-123 inhibits endothelin-1 induced contractions of porcine coronary artery with KB of 40 nM1.
    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 desiccated at -20°C.
    Solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
      • BQ-123 sodium salt
        Alomone Labs BQ-123 sodium salt inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
        Dose-response curve of BQ-123 sodium salt (#B-185) inhibition of the ET-A receptor-mediated, endothelin-1-evoked Ca2+ mobilization. Cells were loaded with Calcium 6 dye, incubated with BQ-123 sodium salt, and stimulated with 15 nM endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    • 1. Moreland, S. (1994) Cardiovasc. Ther. 12, 48.
    • 2. Kowalczyk, A. et al. (2016) Oxid. Med. Cell Longev. 2016, 2356853.
    • 3. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
      • BQ-123 is a cyclic pentapeptide that acts as potent and selective antagonist of endothelin A (ET-A) receptors. BQ-123 exhibits a 1000-fold selectivity for ET-A receptors over ET-B receptors. It antagonizes endothelin-1 radioligand binding to ET-A and ET-B receptors with IC50 values of 22 nM and 18 µM, respectively1.

        Studies show that BQ-123 prevents production of TNF-α and IL-6 in skeletal muscle of LPS-treated rat and enhances antioxidant defense1,2.

        There are two subtypes of endothelin receptor: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle where they mediate vasoconstriction. They are also detected in several regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides3.

    Target ET-A receptors
    Last update: 26/08/2019

    BQ-123 sodium salt (#B-185) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use