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phosphoramidon

Names

[ CAS No. ]:
36357-77-4

[ Name ]:
phosphoramidon

[Synonym ]:
PHOSPHORAMIDON SODIUM SALT
yptophan
phophoramidon
eucyl)
PHOSPHORAMIDON

Biological Activity

[Description]:

Phosphoramidon, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Cardiovascular Disease
Signaling Pathways >> Metabolic Enzyme/Protease >> Angiotensin-converting Enzyme (ACE)
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Metabolic Enzyme/Protease >> MMP
Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin

[Target]

Microbial Metabolite


[In Vitro]

Phosphoramidon (1-500 μM; 30 min) inhibits ET-converting enzyme (ECE) activity in a dose-dependent manner in solubilized rabbit lung membranes[5].

[In Vivo]

Phosphoramidon (0.25 mg/kg per min; i.v.) suppresses the hypertensive effect of big endothelin-1 in rats[4]. Phosphoramidon (1-30 mg/kg; i.v.; once) blocks the pressor activity of porcine big endothelin-1-(1-39) in rats[5]. Animal Model: Male Sprague-Dawley rats[4] Dosage: 0.25 mg/kg per min Administration: Intravenous injection Result: Markedly suppressed the hypertensive effect of big endothelin-1.

Chemical & Physical Properties

[ Density]:
1.48 g/cm3

[ Molecular Formula ]:
C23H34N3O10P

[ Molecular Weight ]:
543.50400

[ Exact Mass ]:
543.19800

[ PSA ]:
220.48000

[ LogP ]:
1.01040

[ Index of Refraction ]:
1.631

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
YN6688000
CHEMICAL NAME :
L-Tryptophan, N-(N-(((6-deoxy-alpha-L-mannopyranosyl)oxy)hydroxypho sphinyl)-L-leucyl)-
CAS REGISTRY NUMBER :
36357-77-4
LAST UPDATED :
199206
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C23-H34-N3-O10-P
MOLECULAR WEIGHT :
543.57

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 26,621,1973

Safety Information

[ Safety Phrases ]:
22-24/25

Precursor & DownStream

Precursor

DownStream

Related Compounds

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