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BQ-3020

A Selective and Potent Endothelin B Receptor Agonist

Cat #: SPE-200
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Synthetic peptide
    MW: 2006 Da
    Purity: ≥98% (HPLC)
    Effective concentration 1 pM -100 nM.
    Sequence LMDKEAVYFAHLDIIW.
    Modifications Leu1 = N-terminal Ac.
    Structure
    Molecular formula C96H140N20O25S1.
    CAS No.: 143113-45-5
    Activity BQ-3020 is a selective and potent ET-B receptor agonist1.
    References-Activity
    1. Ekelund, U. et al. (1994) Br. J. Pharmacol. 112, 887.
    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. 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 BQ-3020 activates Endothelin B receptor-mediated Ca2+ mobilization in CHO-K1-mt Aequorin cells.
      Alomone Labs BQ-3020 activates Endothelin B receptor-mediated Ca2+ mobilization in CHO-K1-mt Aequorin cells.
      Dose-response curve of normalized activation of the Endothelin B receptor-mediated Ca2+ mobilization, evoked by BQ-3020 (#SPE-200). Ca2+ response was detected by measuring aequorin-derived fluorescence following application of BQ-3020 and Endothelin-1 at different concentrations. The EC50 measured for BQ-3020 is 23 pM.
    References - Scientific background
    1. Strachan, F.E. et al. (2000) Br. J. Clin. Pharmacol. 50, 27.
    2. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    3. Xie, C. and Wang, D.H. (2009) Hypertension 54, 1298.
    4. Davenport, A.P. et al. (2016) Pharmacol. Rev. 68, 357.
    Scientific background

    BQ-3020 is a synthetic peptide that acts as a selective and potent ET-B (endothelin B) receptor agonist, a receptor that belongs to the G protein-coupled receptors (GPCR). BQ-3020 is a linear analog of the ET-B receptor ligand endothelin 1 (ET-1), with very close structural similarity to ET-1 compared to other agonists. Several studies have shown that locally active in vivo administration of BQ-3020 causes arterial constriction in healthy human blood vessels1.

    Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-B receptor has high equal affinity for all endothelin isopeptides2. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia3.

    Endothelin receptor agonists are being used as useful tools for the functional characterization of these receptors. Studies have shown that administering ET-B receptor agonist into the rat renal medulla, leads to natriuresis and diuresis via a mechanism that is NOS1-dependent4.

    Target ET-B receptor
    Net Peptide Content: 100%
    Lyophilized Powder
    Last update: 25/04/2021

    BQ-3020 (#SPE-200) is a highly pure, synthetic, and biologically active peptide.

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    For research purposes only, not for human use

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