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Phosphoramidon

Neprilysin inhibitor
 
BML-PI111-0005 5 mg 146.00 USD
 
BML-PI111-0025 25 mg 602.00 USD
 
Replaces Prod. #: ALX-260-011

Inhibits neutral endopeptidase 24.11 (NEP, neprilysin; EC 3.4.24.11) (Ki=2nM), a cell surface zinc metalloprotease which cleaves bioactive peptides such as bradykinin, neurotensin, and enkephalin. Also inhibits neprilysin 2 (Ki~2nM). Potent inhibitor of endothelin-converting enzyme (ECE) (IC50=0.68μM).

Product Specification

Alternative Name:N-(α-Rhamnopyranosyloxyhydroxyphosphinyl)-L-leucyl-L-tryptophan
 
Sequence:N-(α-Rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp . 2Na
 
Formula:C23H34N3O10P . 2Na
 
MW:541.5 . 46.0
 
CAS:119942-99-3
 
Purity:≥97% (HPLC)
 
Appearance:White to slightly yellow solid.
 
Solubility:Soluble in water, DMSO or methanol.
 
Long Term Storage:-20°C
 
Use/Stability:Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months at -20°C.
 
Background / Technical Information:Note: Product is not sterile.
 
BML-PI111 structure
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BML-PI111 structure

Product Literature References

Cell-specific activity of neprilysin 2 isoforms and enzymic specificity compared with neprilysin: C. Rose, et al.; Biochem J. 363, 697 (2002), Abstract;
Neurotensin is metabolized by endogenous proteases in prostate cancer cell lines: T.W. Moody, et al.; Peptides 19, 253 (1998), Abstract;
Neutral endopeptidase and angiotensin-converting enzyme inhibitors increase nitric oxide production in isolated canine coronary microvessels by a kinin-dependent mechanism: X. Zhang, et al.; J. Cardiovasc. Pharmacol. 31, 623 (1998), Abstract;
Soluble human endothelin-converting enzyme-1: expression, purification, and demonstration of pronounced pH sensitivity: K. Ahn, et al.; Arch. Biochem. Biophys. 359, 258 (1998), Abstract;
Almost complete protection from [Met5]-enkephalin-Arg6-Gly7-Leu8 (Met-enk-RGL) hydrolysis in membrane preparations by the combination of amastatin, captopril and phosphoramidon: T. Hiranuma, et al.; J. Pharmacol. Exp. Ther. 281, 769 (1997), Abstract;
Neutral endopeptidase-24.11 inhibitors: from analgesics to antihypertensives?: B.P. Roques & A. Beaumont; TIPS 11, 245 (1990), Abstract;
Phosphoramidon, a metalloproteinase inhibitor, suppresses the hypertensive effect of big endothelin-1: Y. Matsumura, et al.; Eur. J. Pharmacol. 185, 103 (1990), Abstract;
The hydrolysis of alpha-human atrial natriuretic peptide by pig kidney microvillar membranes is initiated by endopeptidase-24.11: S.L Stephenson & A.J. Kenny; Biochem. J. 243, 183 (1987), Abstract;
Letter: A thermolysin inhibitor produced by Actinomycetes: phospholamidon: H. Suda, et al.; J. Antibiot. (Tokyo) 26, 621 (1973), Abstract;

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