1. Metabolic Enzyme/Protease
  2. Angiotensin-converting Enzyme (ACE)
    Neprilysin
  3. Phosphoramidon Disodium

Phosphoramidon Disodium 

Cat. No.: HY-N2021A Purity: >98.0%
Handling Instructions

Phosphoramidon disodium is a metalloprotease inhibitor. Phosphoramidon 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.

For research use only. We do not sell to patients.

Phosphoramidon Disodium Chemical Structure

Phosphoramidon Disodium Chemical Structure

CAS No. : 164204-38-0

Size Price Stock Quantity
10 mM * 1 mL in Water USD 209 In-stock
Estimated Time of Arrival: December 31
1 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 162 In-stock
Estimated Time of Arrival: December 31
10 mg USD 288 In-stock
Estimated Time of Arrival: December 31
25 mg USD 576 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1032 In-stock
Estimated Time of Arrival: December 31
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Description

Phosphoramidon disodium is a metalloprotease inhibitor. Phosphoramidon 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.

IC50 & Target

IC50: 3.5 μM (ECE), 34 nM (NEP), 78 μM (ACE)[1]

In Vitro

Phosphoramidon is a naturally occurring glycopeptide first isolated from a strain of Streptomyces tanashiensis. It has a unique chemical structure featuring a phosphoramidate linkage between a-L-rhamnose and L-leucineL-tryptophan. As a microbial metabolite, phosphoramidon exhibits potent inhibitory activity against thermolysin, a zinc endopeptidase isolated from Bacillus thermoproteolyticus (Ki=32 nM)[2].

In Vivo

Intranasal administration of phosphoramidon produces significantly elevated cerebral Aβ levels in wild-type mice. Furthermore, intranasal phosphoramidon administration in double knockout mice lacking NEP and NEP2 also shows increased levels of Aβ40[3]. Phosphoramidon blocks the formation of endothelin-1 (ET-1), a proinflammatory mediator implicated in the pathogenesis of a variety of lung diseases. Phosphoramidon significantly reduces LPS-induced pulmonary inflammation as measured by lung histology, neutrophil content of bronchoalveolar lavage (BAL) fluid, percent tumor necrosis factor receptor 1 (TNFR1)-labeled BAL macrophages, and alveolar septal cell apoptosis[4]. Phosphoramidon significantly decreased ET-1 levels, causing a concomitant big ET-1 increase and dose-dependently attenuated indomethacin-induced gastric mucosal damage[5].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 140 mg/mL (238.31 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

The Ki values are determined in a 50 mM Tris-HCl, 10 mM CaCl2 buffer (pH 7.5) with FA-Gly-Leu-NH2 (FAGLA) as a substrate by using an Agilent 8453 UV-vis spectrophotometer in triplicate. Henderson plots are employed for the calculation of Ki values. A mixture of buffer (970 μL), phosphoramidon (0-80 nM, 20 μL), and thermolysin (40 nM, 10 μL) is incubated at 25 C for 15 min in a cuvette (2 mL). A solution of FAGLA (0.1-0.5 mM, 1.0 mL) in Tris buffer pH 7.5 is added into the cuvette. The absorbance decrease upon cleavage of FAGLA by thermolysinis recorded at 340 nm wavelength for 5 min. The concentration of thermolysinis determined from the molar extinction coefficient[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3][4]

Mice[3]
Phosphoramidon is dissolved in phosphate-buffered saline (PBS+1 mM ascorbic acid) at a concentration of 30 mM. Anesthetized mice are placed on their backs and eight 3-μL drops of phosphoramidon solution are administered to alternating nares every 2 min. This is done once per day for 5 days. Mice are euthanized under anesthesia for tissue collection 2 h post phosphoramidon administration on day 5. Control mice are treated with intranasal PBS vehicle solution alone. Brains are removed and dissected into the desired brain regions before being homogenized in 5 M guanidine HCl to extract total Aβ. After centrifugation (16,000×g), the supernatants are diluted tenfold and Aβ (1-42 and 1-40) is quantified by specific ELISA.
Rats[4]
Animals are treated with phosphoramidon either intraperitoneally or intratracheally via nebulization. To examine the effects of intraperitoneal administration, animals are injected with 0.5 mg of phosphoramidon dissolved in 0.5 mL of phosphatebuffered saline (PBS). For the nebulization studies, animals are placed in an exposure chamber and treated for 1 hour with an aerosol composed of a 0.1% solution of phosphoramidon dissolved in distilled water. The aerosolized phosphoramidonis delivered through a ceiling port via a Misty-Ox nebulizer attached to an air compressor. Negative pressure is applied by a blower attached to a secondary outflow port to insure proper circulation of the aerosol.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

587.47

Formula

C₂₃H₃₂N₃Na₂O₁₀P

CAS No.

164204-38-0

SMILES

O=C([O-])[[email protected]](CC1=CNC2=CC=CC=C12)NC([[email protected]](CC(C)C)NP([O-])(O[[email protected]]3[[email protected]@H]([[email protected]@H]([[email protected]]([[email protected]](C)O3)O)O)O)=O)=O.[Na+].[Na+]

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Phosphoramidon Disodium
Cat. No.:
HY-N2021A
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Phosphoramidon Disodium

Cat. No.: HY-N2021A