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Submit ReviewAmbrisentan
Description: Selective ETA antagonist
Chemical Name: (αS)-α-[(4,6-Dimethyl-2-pyrimidinyl)oxy]-β-methoxy-β-phenylbenzenepropanoic acid
Purity: ≥99% (HPLC)
Biological Activity for Ambrisentan
Ambrisentan is a selective endothelin receptor ETA antagonist. Displays approximately 200-fold selectivity for ETA over ETB (Ki values are 1 nM and 195 nM for respectively). Prevents endothelin-induced sudden death in rats.
Compound Libraries for Ambrisentan
Ambrisentan is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Ambrisentan
| M. Wt | 378.42 |
| Formula | C22H22N2O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 177036-94-1 |
| PubChem ID | 6918493 |
| InChI Key | OUJTZYPIHDYQMC-LJQANCHMSA-N |
| Smiles | CC1=CC(C)=NC(O[C@H](C(O)=O)C(C2=CC=CC=C2)(OC)C3=CC=CC=C3)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ambrisentan
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.84 | 100 | |
| ethanol | 37.84 | 100 |
Preparing Stock Solutions for Ambrisentan
The following data is based on the product molecular weight 378.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.64 mL | 13.21 mL | 26.43 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.29 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets for Ambrisentan
References for Ambrisentan
References are publications that support the biological activity of the product.
Riechers et al (1996) Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. J.Med.Chem. 39 2123 PMID: 8667356
Vatter & Seifert (2006) Ambrisentan, a non-peptide endothelin receptor antagonist. Cardiovasc.Drug Rev. 24 63 PMID: 16939634
If you know of a relevant reference for Ambrisentan, please let us know.
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Keywords: Ambrisentan, Ambrisentan supplier, endothelin, ETA, receptor, antagonists, inhibits, antagonism, selective, Endothelin, Receptors, 5828, Tocris Bioscience
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