DL-Thiorphan

A thiol containing amido-acid that selectively binds to the active site zinc of metalloproteinases and blocks their activity (IC₅₀ = 2.1 nM for neutral endopeptidase-NEP). Although it is shown to inhibit the activity for Aβ peptide degrading enzyme neprilysin in vitro, it has no effect on the secretion of Aβ peptide or amyloid β precursor protein (APP). Also reported to inhibit the activity of angiotensin-converting enzyme (ACE) at much higher concentrations (IC₅₀ = 140 nM); however, it does not affect the activity of endothelin-converting enzyme.

A thiol-containing amido-acid that selectively binds to the active site zinc of neprilysin (also known as neutral endopeptidase and NEP) and inhibits its activity (IC₅₀ = 2.1 nM). Inhibits the β-amyloid (Aβ) degrading activity of neprilysin in vivo, but does not affect the secretion of either Aβ peptide or amyloid precursor protein (APP). Also shown to inhibit other neprilysin-related family members, such as mouse NL1 (IC₅₀ = 47 nM) and the neprilysin homolog from Ascaris suum (IC₅₀ = 22 µM). Inhibits the activity of angiotensin-converting enzyme (ACE) (IC₅₀ = 140 nM), but has no effect on the activity of endothelin-converting enzyme (ECE).

Cell permeable: no

Primary Target
NEP activity

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2.1 nM for neutral endopeptidase-NEP

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 2 weeks at -20°C.

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