
Biological Activity
Potent, metabolically stable neurotensin receptor agonist peptide (IC50 = 0.15 nM for inhibition of [125I]-NT binding to neonatal mouse brain; EC50 = 1.9 nM for contraction of guinea pig ileum). Produces long-lasting hypothermic, neuroprotective and analgesic effects in mice following central administration in vivo.
Technical Data
M. Wt | 746.96 |
Formula | C38H66N8O7 |
Sequence |
KKPYIL (Modifications: Lys-1 - Lys-2 peptide bond replace with Ψ(CH2-NH)) |
Storage | Desiccate at -20°C |
CAS Number | 139026-66-7 |
PubChem ID | 164415 |
InChI Key | TZCYVPLNMOJUIL-GULBXNHPSA-N |
Smiles | [H]N[C@@H](CCCCN)CN[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(O)=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 water |
Preparing Stock Solutions
The following data is based on the product molecular weight 746.96. 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 | 1.34 mL | 6.69 mL | 13.39 mL |
5 mM | 0.27 mL | 1.34 mL | 2.68 mL |
10 mM | 0.13 mL | 0.67 mL | 1.34 mL |
50 mM | 0.03 mL | 0.13 mL | 0.27 mL |
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References
References are publications that support the products' biological activity.
Lugrin et al (1991) Reduced peptide bond pseudopeptide analogues of neurotensin: binding and biological activities, and in vitro metabolic stability. Eur.J.Pharmacol. 205 191 PMID: 1812009
Dubuc et al (1992) JMV 449: a pseudopeptide analogue of neurotensin-(8-13) with highly potent and long-lasting hypothermic and analgesic effects in the mouse. Eur.J.Pharmacol. 219 327 PMID: 1425958
Torup et al (2003) Neuroprotective effect of the neurotensin analogue JMV-449 in a mouse model of permanent middle cerebral ischaemia. Neurosci.Lett. 351 173 PMID: 14623134
Keywords: JMV 449, supplier, Potent, neurotensin, receptor, agonists, NT, Receptors, JMV449, Neurotensin, Receptors, Neurotensin, Receptors, Tocris Bioscience