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]) |
| Storage | Store at -20°C |
| CAS Number | 148473-36-3 |
| PubChem ID | 5487524 |
| InChI Key | MWZOULASPWUGJJ-NFBUACBFSA-N |
| Smiles | O=C(N[C@@H]([C@H](CC)C)C(N[C@@H](CC(C)C)C(O)=O)=O)[C@H](CC1=CC=CC=C1)CC(NO)=O |
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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References
References are publications that support the products' biological activity.
Doulut et 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
Kitabgi et 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
Menard et 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
Keywords: JMV 390-1, supplier, JMV390-1, endopeptidases, 24.15, 24.11, 24.16, inhibitors, inhibits, neurotensin, neuromedin, n, analgesics, Other, Proteases, Other, Proteases, Tocris Bioscience
