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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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|
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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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.