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[Ala1,3,11,15] Endothelin-1

A Potent Agonist of Endothelin B Receptors 

Cat #: SPE-240
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Synthetic peptide
    MW: 2368 Da
    Purity: ≥98% (HPLC)
    Effective concentration 1 pM -100 nM.
    Sequence ASASSLMDKEAVYFAHLDIIW.
    Structure
    Molecular formula C109H163N25O32S.
    CAS No.: 121204-87-3
    Activity [Ala1,3,11,15 ] Endothelin-1 is a potent ET-B receptor agonist1.
    References-Activity
    1. Nakamichi, K. et al. (1992) Biochem. Biophys. Res. Commun. 182, 144.
    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 Ala[1,3,11,15] Endothelin-1 activates Endothelin B receptor-mediated Ca2+ mobilization in CHO-K1-mt Aequorin cells.
      Alomone Labs Ala[1,3,11,15] Endothelin-1 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  Ala[1,3,11,15] Endothelin-1 (#SPE-240). Ca2+ response was detected by measuring aequorin-derived fluorescence following application of Ala[1,3,11,15] Endothelin-1 and Endothelin-1 at different concentrations. The EC50 measured for Ala[1,3,11,15] Endothelin-1 is 0.38 pM.
    References - Scientific background
    1. Xie, C. and Wang, D.H. (2009) Hypertension 54, 1298.
    2. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    3. Davenport, A.P. et al. (2016) Pharmacol. Rev. 68, 357.
    Scientific background

    [Ala1,3,11,15 ] Endothelin-1 is a potent ET-B (endothelin B) receptor agonist, a receptor that belongs to the G-protein coupled receptor (GPCR) superfamily. [Ala1,3,11,15] Endothelin-1 is a linear synthetic peptide analog of endothelin 1 (ET-1) that shows very high affinity for the receptor. The analog includes a substitution of Ala residue for Cys residues that removes the disulfide bridges that exist in endothelin-11-3.

    Endothelin-1 (ET-1) and its receptor ET-B play an important role in regulating renal function and blood pressure. ET-B Receptor and ET-1 are both expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia1.

    Studies have shown that acute administration of an ET-B receptor agonist into the rat renal medulla leads to natriuresis and diuresis via a mechanism that is NOS1-dependent3.

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

    [Ala1,3,11,15] Endothelin-1 (#SPE-240) 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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