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Atrasentan

(+)-A-127722, A-147627, ABT-627

A Potent and Selective Antagonist of Endothelin A Receptors

Cat #: A-455
Alternative Name (+)-A-127722, A-147627, ABT-627
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 510.62
    Purity: >98%
    Effective concentration 0.01-10 nM.
    Structure
    Chemical name (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid.
    Molecular formula C29H38N2O6.
    CAS No.: 173937-91-2
    PubChem CID 159594
    Activity Atrasentan is a potent and highly selective antagonist of ET-A endothelin receptors, exhibiting a 1000-fold selectivity for ET-A over ET-B receptors, inhibiting endothelin-1 radioligand binding with an IC50 of 0.36 nM and endothelin-1-stimulated phosphoinositol hydrolysis with IC50 of 0.16 nM1.
    References-Activity
    1. Winn, M. et al. (1996) J. Med. Chem. 39, 1039.
    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 products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs Atrasentan inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
      Alomone Labs Atrasentan inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
      Dose-response curve of Atrasentan (#A-455) inhibition of ET-A receptor-mediated, endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 0.124 nM. Cells were loaded with Calcium 6 dye, incubated with Atrasentan, 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. Winn, M. et al. (1996) J. Med. Chem. 39, 1039.
    2. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    Scientific background

    Atrasentan (A-127722) is a synthetic compound that acts as a potent and selective antagonist of endothelin A (ET-A) receptor. Atrasentan is highly selective towards ET-A receptor, exhibiting 1000-fold selectivity over ET-B receptors1. It inhibits endothelin-1 radioligand binding with an IC50 value of 0.36 nM and endothelin-1-stimulated phosphoinositol hydrolysis with an IC50 of 0.16 nM1.

    ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed 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 isopeptides2.

    Target ET-A receptors
    Last update: 06/11/2022

    Atrasentan (#A-455) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

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