| Identification | Back Directory | [Name]
N-[N-[[(6-deoxy-α-L-mannopyranosyl)oxy]hydroxyphosphinyl]-L-leucyl]- L-tryptophan,sodium salt (1:1) | [CAS]
164204-38-0 | [Synonyms]
Phosphoramidon (Disodium)
CRDWMOVRQCMROH-HIKRQZGHSA-N
N-[N-[[(6-Deoxy-α-L-mannopyranosyl)oxy]hydroxyphosphinyl]-L-leucyl]-L-tryptophan disodium salt
N-[N-[[(6-deoxy-α-L-mannopyranosyl)oxy]hydroxyphosphinyl]-L-leucyl]- L-tryptophan,sodium salt (1:1) | [Molecular Formula]
C23H34N3Na2O10P | [MOL File]
164204-38-0.mol | [Molecular Weight]
589.483 |
| Chemical Properties | Back Directory | [storage temp. ]
Desiccate at -20°C | [solubility ]
≥58.7 mg/mL in DMSO; insoluble in EtOH; ≥52.5 mg/mL in H2O | [form ]
solid | [color ]
White to off-white | [Water Solubility ]
Soluble to 100 mM in water |
| Hazard Information | Back Directory | [Description]
Neprilysin (NEP) and NEP2 are membrane-bound zinc metalloproteases. Phosphoramidon is a natural and potent inhibitor of NEP and NEP2, with Ki values of 2 nM for both enzymes. It is also a weak inhibitor of the related zinc metalloprotease endothelin-converting enzyme (Ki = 3.5 μM). Phosphoramidon has little or no effect on a variety of other proteases, including trypsin, papain, chymotrypsin, pepsin, and angiotensin-converting enzyme. | [Uses]
An endothelin-converting enzyme inhibitor, attenuates lipopolysaccharide-induced acute lung injury. | [storage]
Store at -20°C | [References]
[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. |
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