PHOSPHORAMIDON

Description

Phosphoramidon (119942-99-3) inhibits neutral endopeptidase 24.11 (NEP; Neprilysin; EC 3.4.24.11), Ki=2 nM.1?Also inhibits neprilysin 2 (Ki~2 nM).2?Also inhibits endothelin-converting enzyme (IC50?= 0.68 μM).3?Induces a dramatic increase in amyloid-beta levels in rodents.4

The Uses of PHOSPHORAMIDON

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

The Uses of PHOSPHORAMIDON

Phosphoramidon is an inhibitor of NEP 24.11 and NEP2. It is an inhibitor of the enzyme thermolysin, a membrane metallo-endopeptidase inhibitor, and an endothelin converting enzyme inhibitor.

What are the applications of Application

Phosphoramidon is an inhibitor of NEP 24.11 and NEP2

General Description

Phosphoramidon [N-(α-rhamnopyranosyl-oxyhydroxyphosphinyl)-Leu-Trp] is a competitive inhibitor of several soluble zinc metalloproteases. Phosphoramidate is produced naturally by Streptomyces?tanashiensis.

Biochem/physiol Actions

Phosphoramidon can inhibit ZMPSTE24, an integral membrane protein zinc metalloprotease. It is capable of blocking thermolysin.

References

1) Stephenson and Kenny et al. (1987),?The hydrolysis of alpha-human atrial natriuretic peptide by pig kidney microvillar membranes is initiated by endopeptidase-24.11.; Biochem. J.,?243?183. 2) Rose?et al.?(2002),?Cell-specific activity of neprilysin 2 isoforms and enzymic specificity compared with neprilysin; Biochem. J.,?363?697 3) Ahn?et al.?(1998),?Soluble human endothelin-converting enzyme-1: expression, purification, and demonstration of pronounced pH sensitivity; Arch. Biochem. Biphys.,?359?258 4) Marr and Hafez (2014),?Amyloid-beta and Alzheimer’s disease: the role of neprilysin-2 in amyloid-beta clearance; Front. Aging Neurosci.,?6?187