Description: Inhibits multiple neurotensin and neuromedin N degrading enzymes
Chemical Name:N-[(2R)-4-Hydroxyamino)-1,4-dioxo-2-(phenylmethyl)butyl]-L-isoleucyl-L-leucine
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Inhibitor of the major neurotensin and neuromedin N degrading enzymes (IC50 values are 31, 40, 52 and 58 nM for endopeptidase 24.15, endopeptidase 24.11, leucine aminopeptidase and endopeptidase 24.16 respectively). Exhibits analgesic effects in various nociception assays.
Technical Data
M. Wt
449.54
Formula
C23H35N3O6
Sequence
XIL (Modifications: X-1 = N-[(2R)-4-Hydroxyamino)-1,4-dioxo-2-(phenylmethyl)butyl])
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solubility
Soluble to 0.80 mg/ml in sodium bicarbonate (0.01M)
Preparing Stock Solutions
The following data is based on the product molecular weight 449.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.22 mL
11.12 mL
22.24 mL
5 mM
0.44 mL
2.22 mL
4.45 mL
10 mM
0.22 mL
1.11 mL
2.22 mL
50 mM
0.04 mL
0.22 mL
0.44 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Doulutet al (1993) Synthesis and analgesic effects of N-[3-[(hydroxyamino) carbonyl]-1-oxo-2(R)-benzylpropyl]-L-isoleucyl-L-leucine, a new potent inhibitor of multiple neurotensin/neuromedin N degrading enzymes. J.Med.Chem. 36 1369 PMID: 8496905
Kitabgiet al (1992) Effects of thiorphan, bestatin and a novel metallopeptidase inhibitor JMV 390-1 on the recovery of neurotensin and neuromedin N released from mouse hypothalamus. Neurosci.Lett. 142 200 PMID: 1454216
Menardet al (1996) The cytotoxic activity of Bacillus anthracis lethal factor is inhibited by leukotriene A4 hydrolase and metallopeptidase inhibitors. Biochem.J. 320 687 PMID: 8973585