164204-38-0

Neprilysin (NEP) and NEP2 are membrane-bound zinc metalloproteases. Phosphoramidon is a natural and potent inhibitor of NEP and NEP2, with K_i values of 2 nM for both enzymes. It is also a weak inhibitor of the related zinc metalloprotease endothelin-converting enzyme (K_i = 3.5 μM). Phosphoramidon has little or no effect on a variety of other proteases, including trypsin, papain, chymotrypsin, pepsin, and angiotensin-converting enzyme.

An endothelin-converting enzyme inhibitor, attenuates lipopolysaccharide-induced acute lung injury.

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[1]. ikegawa r, matsumura y, tsukahara y, et al. phosphoramidon, a metalloproteinase inhibitor, suppresses the secretion of endothelin-1 from cultured endothelial cells by inhibiting a big endothelin-1 converting enzyme. biochem biophys res commun, 1990, 171(2): 669-675.
[2]. matsumura y, ikegawa r, hisaki k, et al. conversion of big endothelin-1 to endothelin-1 by phosphoramidon-sensitive metalloproteinase derived from aortic endothelial cells. j cardiovasc pharmacol, 1991, 17 suppl 7: s65-7.
[3]. matsuura a, okumura h, ashizawa n, et al. big endothelin-1-induced sudden death is inhibited by phosphoramidon in mice. life sci, 1992, 50(21): 1631-1638.