Avosentan

A Selective Antagonist of Endothelin A Receptors
    Cat #: A-355
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 479.51
    Purity: >99%
    Effective concentration 0.1-100 nM.
      • Avosentan
    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.
    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.
      • Avosentan
        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.
      • 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: 24/01/2020

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

    For research purposes only, not for human use