SB209670

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.
    Structure
    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™.
    References
    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