Description
Endothelin-1 (human, porcine) is an active peptide with strong vasoconstriction effect isolated from the supernatant of cultured porcine aortic endothelial cells. Endothelin 1 has been shown to be present in many mammals, including humans. Although vascular endothelial cells are the main source of endothelin 1, cardiomyocytes, vascular smooth muscle cells, renal tubular epithelial cells and glial cells can all produce endothelin 1, suggesting that endothelin 1 can independently participate in the complex regulatory mechanism of various organs.
Uses
Endothelin-1 (human, porcine) has been used for coating wells in polystyrene ELISA plates. Potent agonist for ETA and ETB endothelia receptors. Induces the production of hypoxia-inducible factor 1α, and, thus, the production of VEGF.
Application
Endothelin-1 (human, porcine) has been used:
to study its effects on the production of erythropoietin under normoxia and carbon monoxide-induced hypoxia in rat models.
as a protein kinase C (PKC) agonist to study its effects on the phosphorylation of myofilament proteins in rat myocytes.
to induce a hypertrophic-like state to study its effects on contraction pressure in normal and mutated human induced pluripotent stem cells (hiPSC)-derived cardiomyocytes.
in vitro hydrolysis products of macroendothelin-1, a precursor of endothelin-1, and their pharmacodynamic properties in rabbits.
as a receptor for endothelin-1 and its role in G protein-mediated signal transduction Research.
Biological Functions
Endothelins are a family of vasoactive peptides secreted
by endothelial cells. The three major endothelin
peptides are all composed of 21 amino acids. Endothelins
are the most potent vasoconstrictors known.
Contraction of vascular smooth muscle in response to
endothelin is associated with an increase in intracellular
calcium. Increases in endothelin levels have been reported
in patients with vasospastic, hypoxic, and ischemic
diseases.The two identified isoforms of endothelin
receptors have differing affinity for the three endothelin
peptides. Selective and nonselective endothelin receptor
antagonists are in development for potential use
in the treatment of hypertension and other disorders associated
with increased vascular resistance.
Biological Activity
Endothelin 1 (human, porcine) is an endogenous potent vasoconstrictor peptide that is an agonist at ETA and ETB receptors. Modulates vascular tone. Endothelin-1 (ET-1) is a potent vasoconstrictor peptide isolated from porcine endothelial cells. ET-1 is widely present at binding sites in blood vessels, heart, kidneys, adrenal glands, lungs, and brain, and its distribution is similar to endothelial cells.
Biochem/physiol Actions
Potent agonist for ETA and ETB endothelin receptors. Induces the production of hypoxia-inducible factor 1α, and, thus, the production of VEGF.
storage
-20°C (desiccate)
