PHOSPHORAMIDON
Synonym(s):N-(α-Rhamno-pyranosyl-oxy-hydroxy-phosphinyl)-Leu-Trp disodium salt;N-(α-Rhamno-pyranosyl-phos-phono)-L -leucyl-L -tryptophan disodium salt
- CAS NO.:119942-99-3
- Empirical Formula: C23H35N3NaO10P
- Molecular Weight: 567.51
- MDL number: MFCD00080262
- EINECS: 252-996-3
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-04-23 13:52:06
What is 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
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.
The Uses of PHOSPHORAMIDON
An endothelin-converting enzyme inhibitor, attenuates lipopolysaccharide-induced acute lung injury.
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
Properties of PHOSPHORAMIDON
storage temp. | -20°C |
solubility | H2O: 1 mM Stock solution stable for 1 month at –20° C. |
form | Solid |
color | White to pale yellow |
BRN | 8105669 |
Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO, methanol, or distilled water may be stored at -20°C for up to 2 months. |
Safety information for PHOSPHORAMIDON
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for PHOSPHORAMIDON
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