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Phosphoramidon Disodium

CAS No. : 164204-38-0

MCE 站：Phosphoramidon Disodium

产品活性：Phosphoramidon Disodium 是金属蛋白酶 (metalloprotease) 抑制剂 。抑制内皮素转化酶 (ECE) ，中性肽内切酶 (NEP) 和血管紧张素转换酶 (ACE) 的IC₅₀ 值分别为 3.5 ，0.034 和 78 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Angiotensin-converting Enzyme (ACE)  |  Neprilysin

In Vitro: Phosphoramidon is a naturally occurring glycopeptide first isolated from a strain of Streptomyces tanashiensis. It has a unique chemical structure featuring a phosphoramidate linkage between a-L-rhamnose and L-leucineL-tryptophan. As a microbial metabolite, phosphoramidon exhibits potent inhibitory activity against thermolysin, a zinc endopeptidase isolated from Bacillus thermoproteolyticus (K_i=32 nM).

In Vivo: Intranasal administration of phosphoramidon produces significantly elevated cerebral Aβ levels in wild-type mice. Furthermore, intranasal phosphoramidon administration in double knockout mice lacking NEP and NEP2 also shows increased levels of Aβ40. Phosphoramidon blocks the formation of endothelin-1 (ET-1), a proinflammatory mediator implicated in the pathogenesis of a variety of lung diseases. Phosphoramidon significantly reduces LPS-induced pulmonary inflammation as measured by lung histology, neutrophil content of bronchoalveolar lavage (BAL) fluid, percent tumor necrosis factor receptor 1 (TNFR1)-labeled BAL macrophages, and alveolar septal cell apoptosis. Phosphoramidon significantly decreased ET-1 levels, causing a concomitant big ET-1 increase and dose-dependently attenuated indomethacin-induced gastric mucosal damage.

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