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Neurotensin is a gut tridecapeptide with many central and peripheral functions, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors(NTR). Neurotensin induces the expression of MIP-2, MCP-1, IL-1β and TNFα in murine microglial cells and stimulates IL-8 secretion in a non-transformed colon epithelial cell line stably transfected with the NTR. The high-affinity NTR, a member of the G-protein coupled receptor (GPCR) family, is present in a majority of human pancreatic and colorectal cancers, suggesting that Neurotensin (NT) may act in an endocrine fashion to affect tumor growth. Acting through the NTR1, Neurotensin is known to stimulate various signal transduction pathways, including intracellular calcium ([Ca2+]i), the mitogen-activated protein kinases (MAPKs), ERK and JNK, and various PKC isoforms. Treatment of HCT116 cells with Neurotensin (100 nM) significantly increases HCT116 cell migration (~3-fold) compared with vehicle treatment.
| Molecular Weight | 1672.92 |
| Formula | C78H121N21O20 |
| CAS Number | 39379-15-2 |
| Solubility (25°C) | Water 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Neurotensin Receptor Products |
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| AF38469
AF38469 |
| Meclinertant
Meclinertant (SR 48692) is an effective, selective, non-peptide and oral antagonist of active neurotensin receptor (NTS1). Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization in human colon cancer cells, with a pA2 value of 8.13. Meclinertant has anti-anxiety, anti-addiction and memory disorder effects. |
| SBI-553
SBI-553 is a potent and effective, brain-penetrant and allosteric modulator of NTR1 with EC50 of 0.34 μM. |
| JMV 449 acetate
JMV 449 acetate is a potent neurotensin receptor agonist. |
| AF40431
AF40431 is the first reported small molecule ligand of sortilin with IC50 of 4.4 µM and Kd of 0.7 µM. AF40431 binds to the neurotensin binding site of sortilin. |
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