598510
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).
别名:
DL-Thiorphan, N-[(RS)-2-Benzyl-3-mercaptopropanoyl]-glycine
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关于此项目
Assay:
≥95% (TLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, desiccated, protect from light
InChI
1S/C12H15NO3S/c14-11(15)7-13-12(16)10(8-17)6-9-4-2-1-3-5-9/h1-5,10,17H,6-8H2,(H,13,16)(H,14,15)
InChI key
LJJKNPQAGWVLDQ-UHFFFAOYSA-N
assay
≥95% (TLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated, protect from light
color
white
solubility
DMSO: 10 mg/mL, ethanol: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
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General description
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).
Biochem/physiol Actions
Cell permeable: no
Primary Target
NEP activity
NEP activity
Product does not compete with ATP.
Reversible: no
Target IC50: 2.1 nM for neutral endopeptidase-NEP
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 2 weeks at -20°C.
Other Notes
Eckman, E.A., et al. 2001. J. Bio. Chem.276, 24540.
Iwata, N., et al. 2001. Science292, 1550.
Shirotani, K., et al. 2001. J. Biol. Chem.276, 21895.
Ghaddar, G., et al. 2000. Biochem. J.347, 419.
Iwata, N., et al. 2000. Nature Med.6, 143.
Takaki, Y., et al. 2000. J. Biochem.128, 897.
Fuller, S.J., et al. 1995. Biochemistry34, 8091.
Sajid, M., et al. 1995. Parasitology.111, 599.
Gomez-Monterrey, I., et al. 1994. J. Med. Chem.37, 1865.
Takahashi, M., et al. 1993. J. Biol. Chem.268, 21394.
Roderick, S.L., et al. 1989. Biochemistry28, 1493.
Iwata, N., et al. 2001. Science292, 1550.
Shirotani, K., et al. 2001. J. Biol. Chem.276, 21895.
Ghaddar, G., et al. 2000. Biochem. J.347, 419.
Iwata, N., et al. 2000. Nature Med.6, 143.
Takaki, Y., et al. 2000. J. Biochem.128, 897.
Fuller, S.J., et al. 1995. Biochemistry34, 8091.
Sajid, M., et al. 1995. Parasitology.111, 599.
Gomez-Monterrey, I., et al. 1994. J. Med. Chem.37, 1865.
Takahashi, M., et al. 1993. J. Biol. Chem.268, 21394.
Roderick, S.L., et al. 1989. Biochemistry28, 1493.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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