| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Neurotensin(8-13) targets the neurotensin receptors, which are G protein-coupled receptors (GPCRs) that include NTS1, NTS2, and NTS3. The compound binds to these receptors with high affinity, mimicking the actions of the full-length neurotensin peptide. NTS1 and NTS2 are the primary mediators of neurotensin's effects, while NTS3 is a sortilin-related receptor with distinct functions. Activation of neurotensin receptors triggers downstream signaling pathways, including Gq/11-mediated phospholipase C activation, Gi/o-mediated adenylate cyclase inhibition, and MAP kinase activation. Neurotensin(8-13) is a valuable tool for studying these signaling pathways and the physiological roles of neurotensin.
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| ln Vitro |
There have been reports of neurotensin (8–13) sensors of neurotensin (NT) depressurization in response to high extracellular adsorption concentrations inhaled. There exist variations in the regeneration of cell surface adsorption [1].
In vitro studies have demonstrated that Neurotensin(8-13) binds to neurotensin receptors with high affinity and activates receptor signaling. The compound's affinity for NTS1 and NTS2 receptors has been characterized using radioligand binding assays, with Ki values in the low nanomolar range. Neurotensin(8-13) has been shown to stimulate calcium mobilization, inhibit adenylate cyclase activity, and activate MAP kinase pathways in cells expressing neurotensin receptors. The compound's in vitro activity is comparable to that of the full-length peptide, making it a useful tool for studying neurotensin receptor pharmacology. |
| ln Vivo |
In vivo studies have demonstrated that Neurotensin(8-13) produces effects similar to those of the full-length neurotensin peptide, including hypothermia, analgesia, and modulation of dopamine signaling. The compound has been shown to produce analgesic effects in animal models of pain and to modulate locomotor activity and reward-related behaviors. Neurotensin(8-13) has also been studied for its potential antipsychotic and neuroprotective effects. However, the compound's in vivo effects are short-lived due to rapid enzymatic degradation, and it is typically administered intracerebroventricularly or by other invasive routes for experimental purposes.
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| Enzyme Assay |
The in vitro receptor binding assay for Neurotensin(8-13) typically involves measuring the compound's affinity for neurotensin receptors using radioligand binding techniques. Membrane preparations from cells expressing NTS1 or NTS2 receptors are incubated with a radiolabeled neurotensin analog and varying concentrations of Neurotensin(8-13). Nonspecific binding is determined in the presence of excess unlabeled ligand. The compound's affinity (Ki value) for the receptors is calculated from competition binding experiments. These assays are standard for characterizing the receptor binding properties of neurotensin analogs.
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| Cell Assay |
Cellular assays for Neurotensin(8-13) are conducted using cell lines expressing neurotensin receptors, such as CHO cells or HEK293 cells transfected with NTS1 or NTS2. Cells are treated with varying concentrations of the peptide, and receptor activation is assessed by measuring calcium mobilization (using calcium-sensitive fluorescent dyes), cAMP accumulation, or MAP kinase activation (using Western blotting or phospho-specific antibodies). The compound's potency (EC50) for receptor activation is determined from dose-response curves. These cell-based assays confirm the compound's activity as a neurotensin receptor agonist and provide information about its signaling properties.
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| Animal Protocol |
In vivo animal studies for Neurotensin(8-13) are conducted in rodent models. The compound is typically administered intracerebroventricularly (ICV) or intrathecally (IT) to bypass the blood-brain barrier, as the peptide does not readily cross it. Effects on pain perception are assessed using standard nociceptive tests, such as the hot plate test or the tail-flick test. Effects on body temperature are measured using rectal thermometers. Effects on locomotor activity are assessed using open field tests. These studies confirm the compound's in vivo activity and help to characterize its pharmacological effects.
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| ADME/Pharmacokinetics |
Neurotensin(8-13) has a short half-life in vivo due to rapid enzymatic degradation by peptidases. The compound is typically administered by injection and produces rapid but short-lived effects. The peptide has a molecular weight of approximately 740.85 and a molecular formula of C36H52N8O9. For research purposes, Neurotensin(8-13) is stored as a lyophilized powder at -20degC and is reconstituted in appropriate buffers before use. The compound's stability in solution is limited, and it should be used promptly after reconstitution. Detailed pharmacokinetic parameters are not available, as the compound is used primarily as a research tool rather than as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Toxicological data for Neurotensin(8-13) are limited. As a research peptide, the compound has not been systematically evaluated for toxicity in preclinical studies. The compound is typically administered in small quantities for experimental purposes, and no significant toxicity has been reported. Standard safety precautions should be followed when handling the compound, and it should be used only for research purposes. The compound is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
Neurotensin(8-13) is a synthetic peptide fragment of neurotensin used primarily as a research tool for studying neurotensin receptor signaling and function. The compound has a molecular formula of C36H52N8O9 and a molecular weight of approximately 740.85. It is a valuable tool for investigating the role of neurotensin in pain modulation, thermoregulation, and dopamine signaling. The compound is not approved for clinical use and is available only for research purposes. It should be handled with appropriate care and used only by trained personnel in laboratory settings.
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| Molecular Formula |
C38H64N12O8
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| Molecular Weight |
816.990360000001
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| Exact Mass |
816.497
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| CAS # |
60482-95-3
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| PubChem CID |
5311318
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| Appearance |
White to off-white solid powder
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| Density |
1.4 g/cm3
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| Index of Refraction |
1.642
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| LogP |
3.479
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
58
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| Complexity |
1430
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](CC1=CC=C(C=C1)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)N
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| InChi Key |
DQDBCHHEIKQPJD-ODKJCKIQSA-N
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| InChi Code |
InChI=1S/C38H64N12O8/c1-5-22(4)30(34(55)48-28(36(57)58)19-21(2)3)49-32(53)27(20-23-12-14-24(51)15-13-23)47-33(54)29-11-8-18-50(29)35(56)26(10-7-17-45-38(42)43)46-31(52)25(39)9-6-16-44-37(40)41/h12-15,21-22,25-30,51H,5-11,16-20,39H2,1-4H3,(H,46,52)(H,47,54)(H,48,55)(H,49,53)(H,57,58)(H4,40,41,44)(H4,42,43,45)/t22-,25-,26-,27-,28-,29-,30-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~61.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 33.33 mg/mL (40.80 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2240 mL | 6.1200 mL | 12.2401 mL | |
| 5 mM | 0.2448 mL | 1.2240 mL | 2.4480 mL | |
| 10 mM | 0.1224 mL | 0.6120 mL | 1.2240 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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