Phosphoramidon Disodium Salt

Short Summary : metalloproteinase inhibitor

Category : Proteases|Other Proteases

Purity : 0.9803

CAS Number : 164204-38-0

Formula : C23H32N3Na2O10P

Molecular Weight :

Molecular Weight : 587.47

SMILE : O=C([O-])[C@@H](NC([C@@H](NP(O[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O)([O-])=O)CC(C)C)=O)CC2=CNC3=C2C=CC=C3.[Na+].[Na+]

Solubility : Soluble in DMSO > 10 mM

Storage : Desiccate at -20°C

Description : Phosphoramidon Disodium Salt is a potent inhibitor of metalloproteinase [1].
Metalloproteinase is an enzyme whose catalytic mechanism involves a metal. Most metalloproteases require zinc and some require cobalt.
Phosphoramidon Disodium Salt is a potent metalloproteinase inhibitor. In porcine aortic endothelial cells, phosphoramidon (10-4 M) inhibited immunoreactive-endothelin (IR-ET) release by 10-20% and increased IR-CTF levels. These results suggested that phosphoramidon reduced the IR-ET release through affecting the conversion of big ET-1 to ET-l [1]. In cultured endothelial cells, phosphoramidon inhibited the increase of ET-1 and C-terminal fragment (CTF) of big ET-1. However, phosphoramidon increased big ET-1 secretion [2].
In anesthetized rats, phosphoramidon inhibited the hypertensive effect of big ET-1 [2]. In mice, phosphoramidon inhibited big ET-1 induced lethality and increased plasma IR-ET-1 through inhibition of the enzyme that converted big ET-1 to ET-1 [3].
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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