Ambrisentan |
| Catalog No.GC17184 |
ETA-receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 177036-94-1
Sample solution is provided at 25 µL, 10mM.
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Ambrisentan is a selective antagonist of ETA-receptor with Ki value of 1nM [1].
Ambrisentan is an orally active diphenyl propionic acid derivative. It is usually used to treat for pulmonary arterial hypertension. In the in vitro assay, ambrisentan shows selective affinity with ETA-receptor over ETB-receptor expressed in CHO cells. The Ki values of ETA- and ETB-receptor are 1nM and 195nM, respectively. This selectivity is much more higher for the recombinant human ET-receptors in intact cells. The Ki values of ETA- and ETB-receptor are 0.63nM and 48.7nM, respectively. As a selective antagonist of ETA-receptor, ambrisentan is preferential to non-selective receptor antagonism as it permitting maintenance of vasodilator and clearance functions specific to ETB- receptors on the endothelial cells. Moreover, ambrisentan also has possible use in the prevention of reperfusion injury and is appropriate to treat for cerebrovascular disorders [1, 2].
References:
[1] Vatter H, Seifert V. Ambrisentan, a Non-peptide Endothelin Receptor Antagonist. Cardiovascular drug reviews, 2006, 24(1): 63-76.
[2] Barst R J. A review of pulmonary arterial hypertension: role of ambrisentan. Vascular health and risk management, 2007, 3(1): 11.
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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