| 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 |
This compound targets the neurotensin receptors NTS1 and NTS2. NTS1 and NTS2 are G-protein coupled receptors that mediate the analgesic and hypothermic effects of neurotensin. The compound shows high affinity for both receptor subtypes, with Ki values in the sub-nanomolar to low-nanomolar range.
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|---|---|
| ln Vitro |
In vitro, (Lys8,Lys9)-Neurotensin (8-13) binds to NTS1 and NTS2 with high affinity. The compound activates these receptors, leading to G-protein coupling and downstream signaling. It is used to study neurotensin receptor pharmacology and the mechanisms of analgesia.
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| ln Vivo |
In vivo, (Lys8,Lys9)-Neurotensin (8-13) exerts analgesic effects through activation of NTS1 and NTS2. The compound can be used for pain relief research. It has been studied as a potential analgesic agent with a mechanism of action distinct from opioid receptors.
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| Enzyme Assay |
Receptor binding assays for this compound use membrane preparations from cells expressing human NTS1 or NTS2. Radiolabeled neurotensin is incubated with varying concentrations of the test peptide, and binding affinity (Ki) is calculated from competition binding curves.
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| Cell Assay |
Cellular assays for this compound typically use cell lines expressing NTS1 or NTS2. Cells are treated with the peptide, and intracellular calcium mobilization or other signaling readouts are measured to confirm receptor activation.
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| Animal Protocol |
In vivo studies with this compound are conducted in rodent models of pain. The peptide is typically administered via intrathecal, intracerebroventricular, or systemic injection. Analgesic effects are assessed using standard pain models such as the hot plate, tail flick, or formalin tests.
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| ADME/Pharmacokinetics |
As a peptide, this compound is expected to have a short half-life due to proteolytic degradation. The compound may be more stable than native neurotensin due to the lysine substitutions at positions 8 and 9. Standard peptide storage conditions apply.
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| Toxicity/Toxicokinetics |
Toxicity data for this compound are limited. Peptide analgesics are generally well-tolerated, though central nervous system effects may occur. Standard safety precautions for laboratory handling of research compounds should be followed.
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| References | |
| Additional Infomation |
This compound is a research-use peptide and is not approved for therapeutic applications. It is also known as JMV438. The peptide is a neurotensin analog used to study neurotensin receptor pharmacology and the development of non-opioid analgesics. It is available from multiple research suppliers.
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| Molecular Formula |
C38H64N8O8
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|---|---|
| Molecular Weight |
760.96400
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| Exact Mass |
760.485
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| CAS # |
139026-64-5
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| PubChem CID |
24868215
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| Appearance |
White to off-white solid powder
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| Density |
1.203 g/cm3
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| Boiling Point |
1109.7ºC at 760 mmHg
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| Flash Point |
624.9ºC
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| LogP |
4.229
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
54
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| Complexity |
1210
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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](CCCCN)NC(=O)[C@H](CCCCN)N
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| InChi Key |
JDVIBJLNEIKOTF-VDXNIVNJSA-N
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| InChi Code |
InChI=1S/C38H64N8O8/c1-5-24(4)32(36(51)44-30(38(53)54)21-23(2)3)45-34(49)29(22-25-14-16-26(47)17-15-25)43-35(50)31-13-10-20-46(31)37(52)28(12-7-9-19-40)42-33(48)27(41)11-6-8-18-39/h14-17,23-24,27-32,47H,5-13,18-22,39-41H2,1-4H3,(H,42,48)(H,43,50)(H,44,51)(H,45,49)(H,53,54)/t24-,27-,28-,29-,30-,31-,32-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2,6-diaminohexanoyl]amino]hexanoyl]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 : ~100 mg/mL (~131.41 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3141 mL | 6.5706 mL | 13.1413 mL | |
| 5 mM | 0.2628 mL | 1.3141 mL | 2.6283 mL | |
| 10 mM | 0.1314 mL | 0.6571 mL | 1.3141 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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