Thiorphan is a potent inhibitor of neprilysin, a membrane metallo-endopeptidase that cleaves peptide hormones, such as enkephalins, glucagon, and bradykinin (Ki = 4-140 nM).{25518,25520,25517} It is much less effective against neprilysin-2 (IC50 = 22.1 μM), angiotensin-converting enzyme, and endothelin-converting enzyme-1.{24072,25518,25520,25517} Thiorphan can be produced in vivo via the metabolism of the prodrug acetorphan.{25519} Neprilysin is overexpressed in many forms of cancer and may play a role in protecting against Alzheimer’s disease.
产品描述
A potent inhibitor of neprilysin, a membrane metallo-endopeptidase that cleaves peptide hormones, such as enkephalins, glucagon, and bradykinin (Ki = 4-140 nM); produced in vivo via the metabolism of the prodrug acetorphan