A Potent Antagonist of Endothelin Receptors
  • New
Cat #: S-205
Sizes: 0.5 mg, 1 mg, 2.5 mg, 5 mg
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 520.53 Da.
    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 number 157659-79-5.
    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.
    Storage before reconstitution Product before reconstitution should be stored at -20oC.
    Reconstitution Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage after reconstitution Up to three months at -20°C.
    Our bioassay
    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™.
    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.
    Target: Endothelin receptors
    Last update: 08/02/2018

    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.

    Alomone Labs is pleased to offer SB209670 (#S-205). 

    For research purposes only, not for human use