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 Details
| Alternative Name: | N-(α-Rhamnopyranosyloxyhydroxyphosphinyl)-L-leucyl-L-tryptophan |
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| Sequence: | N-(α-Rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp . 2Na |
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| Formula: | C23H34N3O10P . 2Na |
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| MW: | 541.5 . 46.0 |
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| CAS: | 119942-99-3 |
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| Purity: | ≥97% (HPLC) |
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| Appearance: | White to slightly yellow solid. |
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| Solubility: | Soluble in water, DMSO or methanol. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| 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. |
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| Technical Info/Product Notes: | Note: Product is not sterile. |
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| Regulatory Status: | RUO - Research Use Only |
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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; Trends Pharmacol. Sci.
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;
