Overview
Alomone Labs is pleased to offer the Endothelin Receptor Antagonist Explorer Kit (#EK-256). The Explorer Kit contains endothelin receptor antagonists, ideal for screening purposes.
Compounds
| Product Name | Cat # | Size |
|---|---|---|
A-192621 |
A-360 | 1 x 1 mg |
ACT-132577 |
A-350 | 1 x 5 mg |
Atrasentan |
A-455 | 1 x 1 mg |
Avosentan |
A-355 | 1 x 5 mg |
BMS 182874 hydrochloride |
B-500 | 1 x 5 mg |
BQ788 |
B-175 | 1 x 0.5 mg |
BQ788 sodium salt |
B-176 | 1 x 0.5 mg |
BQ-123 sodium salt |
B-185 | 1 x 5 mg |
Darusentan |
D-265 | 1 x 5 mg |
FR 139317 |
F-180 | 1 x 5 mg |
IRL 2500 |
I-190 | 1 x 5 mg |
PD-156707 |
P-305 | 1 x 5 mg |
PD-164333 |
P-310 | 1 x 0.5 mg |
Ro46-8443 |
R-185 | 1 x 1 mg |
SB209670 |
S-205 | 1 x 0.5 mg |
Sitaxsentan |
S-186 | 1 x 5 mg |
TAK-044 |
SPE-320 | 1 x 5 mg |
Zibotentan |
Z-130 | 1 x 5 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.
