2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Endothelin-Converting Enzyme (ECE)
  5. ECE-1 Isoform

ECE-1

Endothelin-converting enzyme-1 (ECE-1) functions as a membrane-bound metalloprotease that catalyzes the conversion of big endothelin to active endothelin-1 (ET-1), regulating vascular tone and endothelial function[1][2]. Mechanistically, ECE-1 modulates peptide signaling through endosomal pathways, including degradation of internalized neuropeptides such as somatostatin-14, and interacts with receptor trafficking machinery to control cellular responsiveness[3]. ECE-1 activity is highly relevant in cardiovascular and renal diseases, including systemic hypertension, chronic heart failure, and diabetic nephropathy, as perturbations in ECE-1 expression or activity correlate with pathological ET-1 accumulation[4][5][2]. Four ECE-1 isoforms (ECE-1a, 1b, 1c, and 1d) arise from alternative promoter usage, sharing catalytic domains but differing in cytosolic tails, which dictate subcellular localization and functional specificity; for example, ECE-1b is retained in late endosomes while ECE-1a localizes to the plasma membrane[1]. Heterodimerization among isoforms can modulate enzymatic distribution and extracellular activity, suggesting inter-isoform regulation as a potential therapeutic strategy[1]. Pharmacological studies indicate that selective small-molecule inhibitors, such as SM-19712, can block ECE-1-mediated peptide hydrolysis in acidic endosomes, providing experimental tools for dissecting isoform-specific functions and developing cardiovascular therapeutics[4][3].

ECE-1 Related Products (1):

Cat. No. Product Name Effect Purity
  • HY-120148A
    SM19712
    		Inhibitor 99.0%
    SM19712 is an orally active, selective endothelin converting enzyme (ECE) inhibitor. SM19712 inhibits conversion of big ET-1 to ET-1. SM19712 attenuates colonic angiogenesis, tissue injury, inflammation, without altering colon shortening or myeloperoxidase levels in mice. SM19712 can be used for the research of inflammatory bowel disease (colitis), ischemic acute renal failure, acute myocardial infarction, and myocardial ischemia/reperfusion injury.