Phosphoramidon Disodium Salt |
| Katalog-Nr.GC16768 |
Phosphoramidon-Dinatriumsalz ist ein Metalloprotease-Inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 164204-38-0
Sample solution is provided at 25 µL, 10mM.
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Phosphoramidon Disodium Salt is a potent inhibitor of metalloproteinase [1].
Metalloproteinase is an enzyme whose catalytic mechanism involves a metal. Most metalloproteases require zinc and some require cobalt.
Phosphoramidon Disodium Salt is a potent metalloproteinase inhibitor. In porcine aortic endothelial cells, phosphoramidon (10-4 M) inhibited immunoreactive-endothelin (IR-ET) release by 10-20% and increased IR-CTF levels. These results suggested that phosphoramidon reduced the IR-ET release through affecting the conversion of big ET-1 to ET-l [1]. In cultured endothelial cells, phosphoramidon inhibited the increase of ET-1 and C-terminal fragment (CTF) of big ET-1. However, phosphoramidon increased big ET-1 secretion [2].
In anesthetized rats, phosphoramidon inhibited the hypertensive effect of big ET-1 [2]. In mice, phosphoramidon inhibited big ET-1 induced lethality and increased plasma IR-ET-1 through inhibition of the enzyme that converted big ET-1 to ET-1 [3].
References:
[1]. Ikegawa R, Matsumura Y, Tsukahara Y, et al. Phosphoramidon, a metalloproteinase inhibitor, suppresses the secretion of endothelin-1 from cultured endothelial cells by inhibiting a big endothelin-1 converting enzyme. Biochem Biophys Res Commun, 1990, 171(2): 669-675.
[2]. Matsumura Y, Ikegawa R, Hisaki K, et al. Conversion of big endothelin-1 to endothelin-1 by phosphoramidon-sensitive metalloproteinase derived from aortic endothelial cells. J Cardiovasc Pharmacol, 1991, 17 Suppl 7: S65-7.
[3]. Matsuura A, Okumura H, Ashizawa N, et al. Big endothelin-1-induced sudden death is inhibited by phosphoramidon in mice. Life Sci, 1992, 50(21): 1631-1638.
| Cell experiment [1]: | |
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Cell lines |
ECs isolated from fresh porcine thoracic aortas |
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Preparation method |
The solubility of this compound in DMSO is >10mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10- 7-10-4 M |
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Applications |
In ECs, phosphoramidon (10- 7-10-4 M) suppressed dose-dependently the apparent converting activity of the membrane fraction and suppressed the membrane fraction induced apparent conversion of big ET-l to ET-l ( Endothelin-1 ). ET-l is a 21 amino acid peptide isolated from the culture medium of vascular endothelial cells (ECs), the secretion of ET-l from cultured ECs was abolished by the addition of phosphoramidon. |
| Animal experiment [2]: | |
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Animal models |
Wild-type mice, NEP/NEP2-deficient mice |
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Dosage form |
24 μl (30 mM) once per day for 5 days. |
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Application |
Intranasal administration of phosphoramidon produced significantly elevated cerebral Aβ (Beta-amyloid peptide) levels in wild-type mice. In NEP/NEP2-deficient mice, Aβ levels were significantly elevated by phosphoramidon, in the absence of NEP (Aβ degrading enzymes) and NEP2, phosphoramidon clearly elevates Aβ1–40 levels relative to Aβ1–42 levels. NEP and NEP2 may be the major “NEP-like” Aβ1–42-degrading (phosphoramidon-sensitive) enzymes in the rodent brain. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Matsumura Y, Ikegawa R, Hisaki K., et al. Conversion of big endothelin-1 to endothelin-1 by phosphoramidon-sensitive metalloproteinase derived from aortic endothelial cells. J Cardiovasc Pharmacol, 1991, 17 Suppl 7: S65-7. [2] . Hanson LR., et al. Intranasal phosphoramidon increases beta-amyloid levels in wild-type and NEP/NEP2-deficient mice.J MolNeurosci. 2011 Mar;43(3):424-7. |
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| Cas No. | 164204-38-0 | SDF | |
| Chemical Name | sodium (S)-3-(1H-indol-3-yl)-2-((S)-4-methyl-2-((oxido(((2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)phosphoryl)amino)pentanamido)propanoate | ||
| Canonical SMILES | O=C([O-])[C@@H](NC([C@@H](NP(O[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O)([O-])=O)CC(C)C)=O)CC2=CNC3=C2C=CC=C3.[Na+].[Na+] | ||
| Formula | C23H34N3O10P • 2Na | M.Wt | 589.5 |
| Löslichkeit | 14mg/mL in DMSO; 10 mg/ml in DMF; PBS (pH 7.2): 10 mg/ml | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6964 mL | 8.4818 mL | 16.9635 mL |
| 5 mM | 0.3393 mL | 1.6964 mL | 3.3927 mL |
| 10 mM | 0.1696 mL | 0.8482 mL | 1.6964 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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