|Ambrisentan ETA-receptor antagonist|
Sample solution is provided at 25 µL, 10mM.
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Related Compound Libraries
|Cas No.||177036-94-1||SDF||Download SDF|
|Chemical Name||(2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
Ambrisentan is a selective antagonist of ETA-receptor with Ki value of 1nM .
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].
 Vatter H, Seifert V. Ambrisentan, a Non-peptide Endothelin Receptor Antagonist. Cardiovascular drug reviews, 2006, 24(1): 63-76.
 Barst R J. A review of pulmonary arterial hypertension: role of ambrisentan. Vascular health and risk management, 2007, 3(1): 11.