Ambrisentan is a propanoic acid??based, orally-available, endothelin receptor type A-receptor antagonist for the once-daily treatment of pulmonary arterial hypertension (PAH). It has >4000-fold selectivity for the type A receptor over type B receptor. Studies indicate that Ambrisentan has a low potential for drug interactions and at therapeutic concentrations does not inhibit UDP-glucuronosyltransferases or CYPs, or induce MDR protein 2 or P-gp. (1)In contrast with other similar therapies, Ambrisentan has been shown to have a lower potential for increase of serum-level concentrations of aminotransferases. (2)
Technical information:
| Chemical Formula: | C22H22N2O4 | |
| CAS #: | 177036-94-1 | |
| Molecular Weight: | 378.42 | |
| Purity: | > 98% | |
| Appearance: | white | |
| Chemical Name: | (S)-2-((4,6-dimethylpyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | LU-208075, BSF-208075 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Frampton, JE., Ambrisentan. Am. J. Cardiovasc. Drugs 2011, 11(4), 215-226. Pubmed ID:21623643 |
| 2. | Galie et al., Results of the Ambrisentan in Pulmonary Arterial Hypertension, Randomized, Double-Blind, Placebo-Controlled, Multicenter, Efficacy (ARIES) Study 1 and 2. Circulation, 2008, 117, 3010-3019. Pubmed ID:18506008 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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