CAS 60482-95-3|Neurotensin (8-13) acetate salt
| Common Name | Neurotensin (8-13) acetate salt | ||
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| CAS Number | 60482-95-3 | Molecular Weight | 816.99000 |
| Density | 1.4 g/cm3 | Boiling Point | / |
| Molecular Formula | C38H64N12O8 | Melting Point | / |
| MSDS | USA | Flash Point | / |
Names
| Name | 2-[[2-[[2-[[1-[2-[[2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid |
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| Synonym | More Synonyms |
Neurotensin (8-13) acetate salt BiologicalActivity
| Description | Neurotensin (8-13) is an active fragment of Neurotensin,. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density. |
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| Related Catalog | Signaling Pathways >>Others >>OthersResearch Areas >>Neurological DiseasePeptides |
| Target | NTR1[1] |
| In Vitro | Receptor internalization induced by Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density. The receptor downregulation in response to high extracellular concentrations of the peptide has been described for Neurotensin (NT) in HT-29 cells and in rat primary cultured neurons. Reappearance of the receptors on the cell surface is also different[1]. |
| Kinase Assay | Binding assays are performed on whole HT-29 cells at confluence. A day before the assay, cells (106 cells/0.4 mL, equivalent to 0.3 mg protein) are placed in 48-well plates. A special binding buffer that includes protease inhibitors (50 mM HEPES, 125 mM NaCl, 7.5 mM KCl, 5.5 mM MgCl2, 1 mM EGTA, 5 g/L bovine serum albumin, 2 mg/L chymostatin, 100 mg/L soybean trypsin inhibitor, 50 mg/L bacitracin, pH 7.4) is used for the experiments. In inhibition studies, cells are incubated for 1 h at 37°C in triplicate with 25,000 cpm of 125I-NT and variable concentrations (0.001-3,000 nM) of unlabeled NT(8-13), unlabeled NT-VIII, or NT-VIII labeled with natRe (final volume of 0.2 mL per well). The cells are then washed twice with cold binding buffer and afterward are solubilized with 1N NaOH at 37°C (0.4 mL per well). The activity is determined in a γ-counter. In saturation studies, cells are incubated in triplicate with increasing concentrations (0.1-10 nM) of 99mTc(CO)3NT-VIII for 1 h at 37°C (final volume, 0.2 mL per well). The concentrations of total technetium (99+99mTc) are equivalent to 0.2-20 MBq 99mTc activity per well. After 2 washings with the same binding buffer as before, the cells are then solubilized with 1N NaOH at 37°C (0.4 mL per well). The bound radioactivity is measured in the γ-counter. Nonspecific binding is determined with 1 μM unlabeled NT(8-13)[1]. |
| References | [1]. García-Garayoa E, et al. Preclinical evaluation of a new, stabilized neurotensin(8--13) pseudopeptide radiolabeled with (99m)tc. J Nucl Med. 2002 Mar;43(3):374-83. |
Chemical & Physical Properties
| Density | 1.4 g/cm3 |
|---|---|
| Molecular Formula | C38H64N12O8 |
| Molecular Weight | 816.99000 |
| Exact Mass | 816.49700 |
| PSA | 344.06000 |
| LogP | 3.47920 |
| Index of Refraction | 1.642 |
| InChIKey | DQDBCHHEIKQPJD-ODKJCKIQSA-N |
| SMILES | CCC(C)C(NC(=O)C(Cc1ccc(O)cc1)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(N)CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)O |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
Articles27
More Articles| In vivo behavioral effects of stable, receptor-selective neurotensin[8-13] analogues that cross the blood-brain barrier. Neuropharmacology 48(3) , 417-25, (2005) A set of neurotensin[8-13] (NT[8-13]) analogues (KK1-19) has been evaluated in various pre-clinical assays relevant for further development of these compounds as potential antipsychotics. Initial scre... | |
| The neurotensin fragment AcNT(8-13) inhibits lowering of interstitial fluid pressure in rat trachea. Am. J. Physiol. Heart Circ. Physiol. 283(3) , H933-40, (2002) Injury to soft tissue results in the lowering of interstitial fluid pressure (P(if)), plasma protein extravasation, and increased total tissue volume. In this study, the effects of N-acetyl neurotensi... | |
| Radiolabeling of multimeric neurotensin(8-13) analogs with the short-lived positron emitter fluorine-18. Appl. Radiat. Isot. 65(7) , 818-26, (2007) Three methods for (18)F-labeling of dimeric and tetrameric neurotensin(8-13) derivatives were evaluated with respect to the labeling yield and the required peptide amounts. Labeling using N-succinimid... |
Synonyms
| Neurotensin(8-13) |
