Overview
Endothelin Receptor Agonist Explorer Kit (#EK-255). The Explorer Kit contains endothelin receptor agonists, ideal for screening purposes.
Compounds
| Product Name | Cat # | Size |
|---|---|---|
BQ-3020 |
SPE-200 | 1 x 5 mg |
[Ala1,3,11,15] Endothelin-1 |
SPE-240 | 1 x 5 mg |
IRL-1620 |
SPE-220 | 1 x 5 mg |
Sarafotoxin S6b |
SPE-160 | 1 x 0.1 mg |
Scientific Background
The endothelin system is comprised of three active peptides, ET-1, 2, and 3, which are considered to be very powerful vasoconstrictive substances. In humans, endothelins mediate their actions via two specific G-Protein Coupled Receptors, ETAR and ETBR. Both ETAR and ETBR are present in heart and in human myocardium at similar levels.1,2
The endothelin receptors differ in their ligand specificity. While ETAR has varying affinities for the endothelin isoforms (ET-1 >ET-2>ET-3), ETBR shows no selective affinity.2,3 Subsequent studies have demonstrated the presence of endothelins in vascular as well as in non-vascular cells and tissues, having multiple biological activities.
- Boivin, B. et al. (2003) J. Biol.Chem. 278, 29153.
- Grant, K. et al. (2003) Br. J. Cancer. 88, 163.
- Davenport, A.P. (2002) Pharmacol. Rev. 54, 219.
- Asham, E. et al. (2001) Br. J. Cancer. 85, 1759.
