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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
Citations for Ambrisentan
Citations are publications that use Tocris products.
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Reviews for Ambrisentan
Average Rating: 5 (Based on 1 Review.)
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Ambrisentan.
By
Alejandra Vidal on 01/08/2025
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Tumoral
Cells were incubated with 100 nM ET1 and 1 µM Ambrisentan (AMB) from 0 to 1100 seconds, previously loaded with the Fluo-4 AM probe.Imaging was performed using an inverted microscope (Nikon Eclipse TE300) equipped with a Lambda 10-2 filter wheel system coupled to a digital camera (Retiga R1, QImaging). A plan fluor 40X, NA 0.75 objective was used. Images were acquired by excitation at 494 nm, and emission was captured at 506 nm using the Micro-Manager 1.4 microscopy software.The fluorescence ratio (F) relative to the initial fluorescence (F₀) was plotted as a function of 5-second time intervals.
