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Ambrisentan
- BSF 208075 - Letairis - Volibris- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C22H22N2O4
- MW: 378.42
Description
Ambrisentan is an orally active, non-peptide endothelin A (ETA) receptor antagonist with pharmacological relevance in endothelin-driven vasoconstriction and vascular remodeling.
Endothelin signaling contributes to pulmonary vascular tone, smooth muscle proliferation and cardiovascular pathology. Ambrisentan is used as a reference antagonist in studies of ETA receptor selectivity, pulmonary arterial hypertension biology and vascular pharmacology.
Key Features
- Selective antagonist of the endothelin A receptor
- Blocks ETA-mediated vasoconstrictive signaling
- Clinically validated pulmonary vascular pharmacology
- Non-peptide small-molecule endothelin receptor ligand
Applications
- Endothelin receptor pharmacology
- Pulmonary arterial hypertension research
- Vascular smooth muscle and remodeling studies
- Antagonist reference compound for ETA assays
More Information
| Parent CAS No. | 177036-94-1 |
|---|---|
| Chemical Name | (S)-2-(4,6-dimethylpyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropanoic acid |
| SMILES | C(C1C=CC=CC=1)(C1C=CC=CC=1)(OC)[C@@H](C(=O)O)OC1=NC(C)=CC(C)=N1 |&1:15,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1 |
| InChiKey | OUJTZYPIHDYQMC-LJQANCHMSA-N |
| CID | 6918493 |
| Short Description | ETA antagonist |
References
- H Vatter and V Seifert. Ambrisentan, a non-peptide endothelin receptor antagonist. Cardiovasc Drug Rev 2006, 24 (1), 63–76.
- CC Chong. Ambrisentan: A new, nonsulphonamide, selective endothelin receptor antagonist for the treatment of pulmonary arterial hypertension. PVRI Review 2009, 1, 31-33.
- H Riechers et al. Discovery and Optimization of a Novel Class of Orally Active Nonpeptidic Endothelin-A Receptor Antagonists. J. Med. Chem., 1996, 39(11), 2123–2128.
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