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Ambrisentan

In stock
Catalog No.
B2075
ETA-receptor antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$100.00
In stock
5mg
$80.00
In stock
10mg
$120.00
In stock

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Background

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.

Chemical Properties

StorageStore at -20°C
M.Wt378.42
Cas No.177036-94-1
FormulaC22H22N2O4
Solubility≥18.921mg/mL in DMSO
Chemical Name(2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid
SDFDownload SDF
Canonical SMILESCC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

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