Endothelin - Receptor Agonists

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E7764 Endothelin 1 ≥97% (HPLC), powder Endothelin-1 (ET-1) is a vasoconstrictor, which is increased in plasma and explants of patients with uterine leiomyomas. Thus, uterine fibroids are linked to increased ET-1 levels and hypertension, which is worsened by hypoxic condtions. ET-1 RNAi and Endostar are capable of preventing the progression and invasiveness of PC-3 (prostate cancer) cells. The plasma levels of this peptide are increased in patients with atrial septal defect (ASD), and these levels might help in diagnosis of closure defects. The plasma level of ET-1 is also higher in patients with end-stage renal disease (ESRD), and this is linked to gradual worsening of pulmonary function tests.
Potent agonist for ETA and ETB endothelin receptors. Induces the production of hypoxia-inducible factor 1α, and, thus, the production of VEGF.
human ... EDN1(1906)
E6877 [Ala1,3,11,15]-Endothelin 1 Selective agonist for ETB endothelin receptors.
human ... EDNRB(1910)
mouse ... EDNRB(13618)
rat ... EDNRB(50672)
E9012 Endothelin 2 human ≥97% (HPLC), powder Endothelin-2 (ET-2) has a regulatory role in multiple cancer types, such as breast and clear cell renal cell carcinoma (ccRCC). It is overexpressed during early stages of non-metastasized ccRCC, and is thought have a role in the progression of the same. It is a hypoxia-related factor, and might have protective action against cell death in neuronal diseases. It acts as a ligand for ET-A and ET-B receptors, which results in vasoconstriction. A985 polymorphism in this gene is thought play a protective role in cardiovascular diseases, but it acts as a susceptibility factor in atrial fibrillation in hypertrophic cardiomyopathy patients. In neural retina, it suppresses angiogenesis, and facilitates the tip cell state in endothelial cells.
human ... EDN2(1907)
E9137 Endothelin 3 human, rat ≥97% (HPLC), powder Endothelin 3 (ET3) is a vasoconstrictor that acts in a paracrine and autocrine manner, and in intestinal lamina propria causes the degranulation of mast cells. It results in the release of ions from intestinal epithelial cells. In acute and chronic intestinal inflammation, it is overexpressed. It is also up-regulated in colon carcinoma, where it supports cell proliferation and survival. It might be involved in colon homeostasis, and is essential for the survival and proliferation of goblet cells. In mice, it is essential for the development of pigment cells derived from neural crest (NC). Its expression is de-regulated in metastatic melanoma.
Potent vasoconstrictor from vascular endothelial cells; preferred agonist for ETB endothelin receptors. Induces the production of VEGF.
human ... EDN3(1908)
rat ... Edn3(366270)
S1522 Sarafotoxin S6a1 ≥97% (HPLC)    
S6545 Sarafotoxin S6c ≥97% (HPLC) Sarafotoxin S6c is an endothelin ETB agonist. It is a peptide isotoxin with strong vasoconstrictor activity, obtained from the Middle Eastern snake, Atractaspis engaddensi. The toxin is composed of 21 amino acids.
human ... EDNRB(1910)
mouse ... EDNRB(13618)
rat ... EDNRB(50672)