Phosphoramidon
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.
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- CAS. Nr.: 36357-77-4
- Formel: C23H34N3O10P
- Molecular Weight:543.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Microbial Metabolite |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
1.2 μM
Compound: 1
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Inhibitory activity was assessed on CHO cells expressing recombinant human Endothelin-converting enzyme 1 (ECE-1).
Inhibitory activity was assessed on CHO cells expressing recombinant human Endothelin-converting enzyme 1 (ECE-1).
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[PMID: 9554884] |
Phosphoramidon (1-500 μM; 30 min) inhibits ET-converting enzyme (ECE) activity in a dose-dependent manner in solubilized rabbit lung membranes[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Phosphoramidon (1-30 mg/kg; i.v.; once) blocks the pressor activity of porcine big endothelin-1-(1-39) in rats[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[4]
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Dosage:0.25 mg/kg per min
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Administration:Intravenous injection
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Result:Markedly suppressed the hypertensive effect of big endothelin-1.
Chemical Information
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CAS. Nr. 36357-77-4
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Molecular Weight 543.50
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Formel C23H34N3O10P
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SMILES
O[C@H]([C@@H]([C@H]([C@@H](O1)C)O)O)[C@@H]1OP(N[C@@H](CC(C)C)C(N[C@H](C(O)=O)CC2=CNC3=CC=CC=C23)=O)(O)=O
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Structure Classification
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Initial Source
Streptomyces tanashiensis
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[3]. Kukkola PJ, et al. Differential structure-activity relationships of phosphoramidon analogues for inhibition of three metalloproteases: endothelin-converting enzyme, neutral endopeptidase, and angiotensin-converting enzyme.J CardiovascPharmacol. 1995;26Suppl 3:S65-8. [Content Brief]
[4]. Matsumura Y, et al. Phosphoramidon, a metalloproteinase inhibitor, suppresses the hypertensive effect of big endothelin-1. Eur J Pharmacol. 1990 Aug 21;185(1):103-6. [Content Brief]
[5]. McMahon EG, et al. Phosphoramidon blocks the pressor activity of porcine big endothelin-1-(1-39) in vivo and conversion of big endothelin-1-(1-39) to endothelin-1-(1-21) in vitro. Proc Natl Acad Sci U S A. 1991 Feb 1;88(3):703-7. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Phosphoramidon Related Classifications
HY-N2021 Related Classifications
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