- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 164204-38-0] Phosphoramidon Disodium
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-N2021A |
| Brand: | MCE |
| CAS: | 164204-38-0 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 587.47 |
| Molecular Formula | C23H32N3Na2O10P |
| SMILES | O=C([C@@H](NC([C@@H](NP(O[C@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](O1)C)(O[Na])=O)CC(C)C)=O)CC2=CNC3=CC=CC=C23)O[Na] |
Summary
Phosphoramidon Disodium, a microbial metabolite , is a specific metalloprotease thermolysin inhibitor with an IC 50 of 0.4 μg/mL. Phosphoramidon Disodium also inhibits endothelin-converting enzyme ( ECE ), neutral endopeptidase ( NEP ), and angiotensin-converting enzyme ( ACE ) with IC 50 values of 3.5, 0.034, and 78 μM, respectively [1] [2] [3] .
IC50 & 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Source
Streptomyces tanashiensis
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 170.22 mM ; Need ultrasonic)
DMSO : 100 mg/mL ( 170.22 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7022 mL | 8.5111 mL | 17.0221 mL |
| 5 mM | 0.3404 mL | 1.7022 mL | 3.4044 mL |
| 10 mM | 0.1702 mL | 0.8511 mL | 1.7022 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (170.22 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution
References
- [1] Umezawa S, , et al. A new microbial metabolite phosphoramidon (isolation and structure). Tetrahedron Letters, 1972, 13(1): 97-100.
- [2] Suda H, et al. A thermolysin inhibitor produced by actinomycetes: phosphoramidon. The Journal of antibiotics, 1973, 26(10): 621-623.
- [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.
- [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.
- [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.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.