Ambrisentan
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.
Storage | Store at -20°C |
M.Wt | 378.42 |
Cas No. | 177036-94-1 |
Formula | C22H22N2O4 |
Solubility | insoluble in H2O; ≥18.92 mg/mL in DMSO; ≥2.85 mg/mL in EtOH with ultrasonic |
Chemical Name | (2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid |
SDF | Download SDF |
Canonical SMILES | CC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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