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BQ788

A Selective Antagonist of Endothelin B Receptors

Cat #: B-175
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 641.81
    Purity: >95%
    Effective concentration 10-100 nM.
    Structure
    Chemical name (2R)-2-[[(2R)-2-[[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]-3-(1-methoxycarbonylindol-3-yl)propanoyl]amino]hexanoic acid.
    Molecular formula C34H51N5O7.
    CAS No.: 173326-37-9
    PubChem CID 5311032
    Activity BQ788 is a potent and highly specific ET-B receptor antagonist, exhibiting selectivity for ET-B over ET-A human receptors when inhibiting the binding of [125I]-Endothelin-1 (IC50 of 1.2 nM and 1300 nM, respectively)1.
    References-Activity
    1. Okada, M. and Nishikibe, M. (2002) Cardiovasc. Drug Rev. 20, 53.
    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 Soluble in DMSO and ethanol. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs BQ788 inhibits ET-B receptor-mediated Ca2+ mobilization in CHO cells.
      Alomone Labs BQ788 inhibits ET-B receptor-mediated Ca2+ mobilization in CHO cells.
      Dose-response plot of BQ788 (#B-175) inhibition of ET-B receptor-mediated, endothelin-1-evoked Ca2+ mobilization (IC50 = 6.57 nM). Cells were loaded with Calcium 6 dye, incubated with BQ788, and stimulated with 30 nM endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Okada, M. and Nishikibe, M. (2002) Cardiovasc. Drug Rev. 20, 53.
    2. Maguire, J.J. and Davenport, A.P. (2015) Semin. Nephrol. 35, 125.
    Scientific background

    BQ788 is a synthetic modified tripeptide that acts as a potent, selective and competitive antagonist of the ET-B (endothelin B) receptor, a receptor that belongs to the G-protein coupled receptor (GPCR) superfamily. BQ788 is a soluble compound that does not bind plasma proteins and is metabolized in a short period of time. It lacks oral bioavailability and requires intra-arterial administration. The compound is used in vitro and in vivo to demonstrate the role of endogenous and exogenous endothelin receptor subtypes in physiological and pathophysiological conditions1,2. It displays IC50 values of 1.2 nM in radiolabeled Girardi heart cells and 1300 nM in human neuroblastoma cell line, respectively1.

    ET-A and ET-B receptors are widely distributed in vascular tissues where they mediate vasoconstriction and in nonvascular tissues such as the liver, kidney, and brain. ET-A receptors have high affinity for ET-1 and ET-2 peptides and relatively low affinity for ET-3, while ET-B receptors show high affinity for all ET isopeptides1.

    Target ET-B receptor
    Last update: 06/11/2022

    BQ788 (#B-175) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Citations

    Citations
    in vivo
    1. Mouse (topical application).
      Nakahara, T. et al. (2010) Sci. Rep. 10, 9510.

    Specifications

    Scientific Background

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