Endothelin-1 (ET-1) is a potent vasoconstrictor that is secreted by vascular endothelial cells. ET-1, ET-2, ET-3, and endothelin β are members
of a family of related peptides. All are 21 amino acid peptides with two disulfide bridges. ET-1 and ET-2 differ by only two residues, while
ET-3 differs from both by six residues. ET-1 and ET-2 are highly effective on vascular smooth muscle, while the effects of ET-3 are minimal.
ET-1 and its precursor, big ET-1, are the primary forms present in the circulation. Circulating ET-1 plays a pathologic role in the etiology of
hypertension and antagonists are utilized in the treatment of this disease. The ET-1 receptor is a seven-transmembrane-domain receptor of the
G-protein-coupled family that signals via transient increases in intracellular Ca2+. It is primarily expressed in lung and heart and is detected at
lower levels in liver, brain, muscle, and kidney. ET-1 receptor interacts with ET-1, ET-2, and ET-3. However, it has a 2-3 fold higher affinity
for ET-1 than ET-2 and the affinity for ET-3 is more than 100 fold lower. Thus, ligation of the ET-1 receptor by ET-1 induces increased
intracellular Ca2+ that signals to promote vasoconstriction.
原厂资料:
注意事项:
1.Since applications vary, each investigator should titrate the reagent to obtain optimal results.
2.Caution: Sodium azide yields highly toxic hydrazoic acid under acidic conditions. Dilute azide compounds in running water before discarding to avoid accumulation of potentially explosive deposits in plumbing.