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 No.: 36357-77-4
- Formule: C23H34N3O10P
- Masse moléculaire:543.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Microbial Metabolite |
Cellular Effect
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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] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
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 No. 36357-77-4
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Masse moléculaire 543.50
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Phosphoramidon Related Classifications
HY-N2021 Related Classifications
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