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G-Protein Coupled Receptors >> Endothelin Receptors >> Antagonists

SB209670

A Potent Antagonist of Endothelin Receptors
  • New
    New
  • Bioassay tested
    Bioassay tested
  • Shipped at room temp.
    Shipped at room temp.
  • Cat #: S-205
  • Size: 0.5 mg, 1 mg, 2.5 mg, 5 mg
  • Source: Synthetic
  • MW: 520.53 Da.
  • Target: Endothelin receptors
General information
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). 
Our Bioassay
Specifications
References
 
Our bioassay
SB209670 - 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™.
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