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A Potent Antagonist of Endothelin Receptors

Cat #: S-205
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 520.53
    Purity: >95%
    Effective concentration 0.2-20 nM.
    Chemical name (1S,2R,3S)-1-(1,3-benzodioxol-5-yl)-3-[2-(carboxymethoxy)-4-methoxyphenyl]-5-propoxy-2,3-dihydro-1H-indene-2-carboxylic acid.
    Molecular formula C29H28O9.
    CAS No.: 157659-79-5
    PubChem CID 108002
    Activity SB209670 is a potent mixed antagonist of ET-A and ET-B Endothelin receptors, shown to inhibit Endothelin-1 radioligand binding to human ET-A and ET-B with Ki of 0.2 nM and 18 nM, respectively. SB209670 inhibits Endothelin-1-evoked vasoconstriction in isolated vascular tissues in vitro, and is orally bioavailable and active in vivo1.
    1. Ohlstein, E.H. et al. (1994) Proc. Natl. Acad. Sci. U.S.A. 91, 8052.
    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 SB209670 inhibits ETA receptor-mediated Ca2+ mobilization in CHO cells.
      Alomone Labs SB209670 inhibits ETA receptor-mediated Ca2+ mobilization in CHO cells.
      Dose response curve of SB209670 (#S-205) inhibition of ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 0.91 nM. Cells were loaded with Calcium 6 dye, incubated with SB209670, 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. Ohlstein, E.H. et al. (1994) Proc. Natl. Acad. Sci. U.S.A. 91, 8052.
    2. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    3. Xie, C. and Wang, D.H. (2009) Hypertension 54, 1298.
    Scientific background

    SB209670 is a nonpeptide synthetic compound that acts as a potent and specific antagonist of endothelin A (ET-A) and B (ET-B) receptors. Intravenous or intraduodenal administration of SB209670 can produce concentration-dependent inhibition of ET-1-mediated vasoconstriction in isolated vascular tissues. Studies on hypertensive rats show that SB209670 produces a dose-dependent decrease in blood pressure. In a gerbil stroke model SB209670 is protective in ischemia-induced neuronal degeneration. Thus, SB209670 can be used as a useful tool in characterizing and classifying the physiological and pathophysiological roles of Endothelin receptors1.

    ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also present in several different regions of the brain. 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 ganglia.

    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 equally for all endothelin isopeptides2,3.

    Target Endothelin receptors
    Last update: 06/11/2022

    SB209670 (#S-205) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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