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

Bosentan hydrate

An Antagonist of Endothelin Receptors
Ro 47-0203
  • New
    New
  • Bioassay tested
    Bioassay tested
  • Shipped at room temp.
    Shipped at room temp.
  • Cat #: B-170
  • Size: 25 mg, 50 mg, 100 mg, 250 mg
  • Source: Synthetic
  • MW: 569.63 Da.
  • Target: Endothelin receptors
General information


Bosentan hydrate (Ro 47-0203), is a synthetic nonpeptide compound that acts as an antagonist of endothelin A (ET-A) and endothelin B (ET-B) receptors. Bosentan hydrate is obtained by structural optimization of Ro 46-2005, a less potent ET-A/ET-B antagonist that is orally bioavailable and active in vivo. Bosentan hydrate competitively inhibits the specific binding of radioligand endothelin-1 to ET-A receptors in human smooth muscle cells with Ki value of 4.7 nM, and to ET-B receptors in human placenta with a Ki of 95 nM1. Bosentan may be used as a useful drug in the management of clinical disorders associated with vasoconstriction1,2.
 
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.
 
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 ET-B receptor has high affinity equally for all endothelin isopeptides3,4.  

Alomone Labs is pleased to offer Bosentan hydrate (#B-170). 
Our Bioassay
Specifications
References
 
Our bioassay
Bosentan_hydrate - Alomone Labs Bosentan hydrate inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
Alomone Labs Bosentan hydrate inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
Dose response curve of Bosentan hydrate (#B-170) inhibition of ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 8.18 nM. Cells were loaded with Calcium 6 dye, incubated with Bosentan hydrate, 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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For research purposes only, not for human use
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