BQ-788 sodium salt |
| Catalog No.GC15916 |
ET B-receptor antagonist,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 156161-89-6
Sample solution is provided at 25 µL, 10mM.
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BQ-788 is a potent and selective antagonist of endothelin (ET) B-receptor with IC50 value of 1.2nM [1].
In the in vitro assay, BQ-788 prevents ET-1 from binding to ETB receptors in human Girardi heart cells with IC50 value of 1.2nM. The inhibition to ETA receptors is much weaker with IC50 value of 1300nM. BQ-788 also inhibits ET binding to ETB receptors with IC50 values of 0.9nM and 1.2nM in porcine cerebellar membranes and hGH cells, respectively. The inhibition effects are quite poor in pCASM cells and SK-N-MC cells with IC50 values of 280nM and 1300nM, respectively. BQ-788 is specific to ET receptors. It cannot significantly inhibit other peptide hormone receptors at concentration of 10μM. It is found that BQ-788 interacts with ETB receptors competitively in hGH cells. Moreover, the in vivo assay demonstrates that ETB receptors are responsible for ET-1-elicited bronchoconstriction in guinea pigs [1].
References:
[1] Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.
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