Endothelin-1 is a peptide vasoconstrictor and agonist of endothelin (ET) receptors ETA and ETB (IC50s = 0.15 and 0.12 nM, respectively).1,2 It induces contraction of pig coronary artery strips (EC50 = 0.52 nM), vasoconstriction of pig cardiac ventricular membrane (120% of control), and increases mean early pressor phase blood pressure by 66 mg Hg in rats when administered at a dose of 1 nmol/kg. In an inducible system of endothelium-restricted overexpression of human endothelin-1, induction of endothelin-1 increases blood pressure in mice.3 It stabilizes and induces nuclear translocation of hypoxia-inducible factor 1 and 2 alpha (HIF-1α and HIF-2α) via ETB in human lymphatic endothelial cells.4 Endothelin-1 autocrine and paracrine signaling modulates cell proliferation, apoptosis, migration, and epithelial-to-mesenchymal transition, suggesting a role in cancer.5WARNING This product is not for human or veterinary use.
