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Avosentan

A Selective Antagonist of Endothelin A Receptors
Cat #: A-355
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 479.51
    Purity: >99%
    Effective concentration 0.1-100 nM.
    Structure
    Chemical name N-[6-methoxy-5-(2-methoxyphenoxy)-2-pyridin-4-ylpyrimidin-4-yl]-5-methylpyridine-2-sulfonamide.
    Molecular formula C23H21N5O5S.
    CAS No.: 290815-26-8.
    PubChem CID 9912992
    Activity Avosentan is a selective antagonist of ET-A endothelin receptors, shown to significantly inhibit endothelin-1-induced contractions in isolated porcine ciliary arteries at 10 nM-1 µM1.
    References-Activity
    1. Konieczka, K. et al. (2011) Curr. Eye Res. 36, 118.
    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 Avosentan inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
      Alomone Labs Avosentan inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
      Dose-response curve of Avosentan (#A-355) inhibition of ET-A receptor-mediated, endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 2.79 nM. Cells were loaded with Calcium 6 dye, incubated with Avosentan, 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. Konieczka, K. et al. (2011) Curr. Eye Res. 36, 118.
    2. Baltatu, O.C. et al. (2012) Front. Physiol. 3, 103.
    3. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    Scientific background

    Avosentan is a synthetic compound that acts as a selective antagonist of endothelin A (ET-A) receptors. It was initially developed for the treatment of diabetic nephropathy1,2. Studies show that inhibition of ET-A receptors can be protective in chronic kidney disease through several processes including vasodilation, attenuation of proteinuria, and increasing diuresis2.

    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 isopeptides3.

    Target ET-A receptors
    Last update: 23/08/2020

    Avosentan (#A-355) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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