Neurotensin(8-13) |
Catalog No.GC36729
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Neurotensin(8-13) is the core active fragment of neurotensin and functions as a biologically active neurotensin receptor (NTSR1) agonist. By binding to NTSR1 with high affinity (Kd≈1–10nM), Neurotensin(8-13) activates the Gq/11 protein signaling pathway, thereby regulating intracellular calcium ion concentration and the activity of protein kinase C (PKC).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 60482-95-3
Sample solution is provided at 25 µL, 10mM.
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Neurotensin(8-13) is the core active fragment of neurotensin and functions as a biologically active neurotensin receptor (NTSR1) agonist. By binding to NTSR1 with high affinity (Kd≈1–10nM), Neurotensin(8-13) activates the Gq/11 protein signaling pathway, thereby regulating intracellular calcium ion concentration and the activity of protein kinase C (PKC)[1-2]. Neurotensin(8-13) can be used in research related to pain management, psychiatric disorders (such as schizophrenia and depression), and tumor-targeted therapy[3-4].
In vitro, human colon adenocarcinoma HT-29 cells were treated with Neurotensin(8-13) (3–100nM) for 1–2 hours. Neurotensin(8-13) significantly induced rapid internalization mediated by the neurotensin receptor NTR1 and caused a time-dependent downregulation of NTR1 receptors on the cell surface[5]. Human non-small cell lung cancer cells NCI-H1299 were treated with Neurotensin(8-13) (100nM) for 2.5 minutes, which significantly induced tyrosine phosphorylation of focal adhesion kinase (FAK). After treating NCI-H1299 cells with Neurotensin(8-13) (10nM) for 24 hours, Neurotensin(8-13) promoted the proliferation of NCI-H1299 cells[6].
In vivo, normotensive rats were injected via the femoral vein with Neurotensin(8-13) (0.1–100nmol/kg). Neurotensin(8-13) dose-dependently reduced diastolic and systolic blood pressure without altering heart rate and showed no direct vasodilatory effect on isolated rat aortic rings[7]. Male Long-Evans rats received microinjections of Neurotensin(8-13) (3nmol in 0.5μl) into the ventral midbrain tegmental area. Neurotensin(8-13) significantly enhanced the reward effect of brain stimulation in the midbrain central gray matter 15–55 minutes after injection[8].
References:
[1] Gilbert JA, McCormick DJ, Pfenning MA, et al. Neurotensin(8-13): comparison of novel analogs for stimulation of cyclic GMP formation in neuroblastoma clone N1E-115 and receptor binding to human brain and intact N1E-115 cells. Biochem Pharmacol. 1989 Oct 1;38(19):3377-82.
[2] Cocioabă D, Fonseca AI, Leonte R, et al. Neurotensin (8-13) and Neuromedin N Neuropeptides Radiolabelling with Copper-64 Produced on Solid or Liquid Targets. Molecules. 2024 Mar 20;29(6):1390.
[3] Li XM, Von Euler G, Hedlund PB, et al. The C-terminal neurotensin-(8-13) fragment potently modulates rat neostriatal dopamine D2 receptors. Eur J Pharmacol. 1993 Mar 30;234(1):125-8.
[4] Pinnock RD, Woodruff GN. The non-peptide neurotensin receptor antagonist SR48692 is not a potent antagonist of neurotensin(8-13) responses of rat substantia nigra neurones in vitro. Neurosci Lett. 1994 May 19;172(1-2):175-8.
[5] García-Garayoa E, Bläuenstein P, Bruehlmeier M, 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.
[6] Leyton J, Garcia-Marin L, Jensen RT, et al. Neurotensin causes tyrosine phosphorylation of focal adhesion kinase in lung cancer cells. Eur J Pharmacol. 2002 May 10;442(3):179-86.
[7] Di Paola ED, Richelson E. Cardiovascular effects of neurotensin and some analogues on rats. Eur J Pharmacol. 1990 Jan 17;175(3):279-83.
[8] Rompré PP, Gratton A. Mesencephalic microinjections of neurotensin-(1-13) and its C-terminal fragment, neurotensin-(8-13), potentiate brain stimulation reward. Brain Res. 1993 Jul 9;616(1-2):154-62.
| Cell experiment [1]: | |
Cell lines | NCI-H1299 cells (human non-small cell lung cancer cell line) |
Preparation Method | NCI-H1299 cells were maintained in RPMI-1640 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with Neurotensin(8-13) at concentrations ranging from 1nM to 1μM for 2.5 minutes to 24 hours. |
Reaction Conditions | 1nM to 1μM; 2.5 minutes to 24 hours |
Applications | Neurotensin(8-13) induced transient tyrosine phosphorylation of focal adhesion kinase (FAK) in NCI-H1299 cells, with maximal phosphorylation observed 1–2.5 minutes after treatment. This effect was specific to the C-terminal fragment. The tyrosine phosphorylation was inhibited by the nonpeptide neurotensin receptor antagonist SR48692 (10μM). Neurotensin(8-13) also bound with high affinity to NCI-H1299 cells (IC₅₀=10nM) and stimulated clonal growth in soft agar assays, while SR48692 suppressed proliferation. |
| Animal experiment [2]: | |
Animal models | Normotensive rats |
Preparation Method | Rats were anesthetized with Pentobarbital (55mg/kg; i.p.), and a cannula was inserted into the femoral vein for peptide administration. Neurotensin(8-13) was dissolved in 0.9% NaCl and injected intravenously at doses ranging from 0.1 to 100nmol/kg. Blood pressure and heart rate were monitored via the carotid artery. |
Dosage form | 0.1–100nmol/kg; i.v.; Single injection. |
Applications | Neurotensin(8-13) induced a dose-dependent decrease in diastolic blood pressure (ED₅₀=6.0nmol/kg) without altering heart rate. At higher doses (≥3nmol/kg), Neurotensin(8-13) elicited a triphasic depressor-pressor-depressor response, with effects lasting over 40 minutes at the highest dose (100nmol/kg). Tachyphylaxis was observed upon repeated administration. |
References: | |
| Cas No. | 60482-95-3 | SDF | |
| Formula | C38H64N12O8 | M.Wt | 816.99 |
| Solubility | Water: 50 mg/mL (61.20 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.224 mL | 6.12 mL | 12.2401 mL |
| 5 mM | 244.8 μL | 1.224 mL | 2.448 mL |
| 10 mM | 122.4 μL | 612 μL | 1.224 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)