Phosphoramidon . disodium salt

Phosphoramidon is a potent, reversible and competitive inhibitor of multiple soluble and membrane-bound zinc metalloproteases, particularly gluzincins, such as neutral endopeptidase NEP (Neprilysin, CD10, EC 3.4.24.11) (Ki = 2nM), NEP2 (Neprilysin-2) (Ki ~ 2nM), or endothelin-converting enzyme (ECE) (IC50 = 0.68µM). It inhibits the thermostable neutral metalloproteinase enzyme thermolysin and the integral membrane protein zinc metalloprotease ZMPSTE24. It has little or no effect on a variety of other proteases, including trypsin, papain, chymotrypsin, pepsin and angiotensin-converting enzyme. Shows anti-inflammatory, anti-neurodegenerative and cardioprotective properties. Blocks through NEP degradation of amyloid beta peptides and increases Abeta levels in rodents, indicating that abnormal amyloid processing in Alzheimer's disease may be carried out by a metalloendopeptidase. Plays also a role in the regulation of neuropeptide signaling and in the metabolism of bioactive peptides, such as bradykinin, neurotensin and enkephalin, via plasma membranes. Blocks the formation of endothelin-1, a proinflammatory mediator implicated in the pathogenesis of a variety of lung diseases.