| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Naltriben mesylate targets the δ2-opioid receptor, a subtype of the δ-opioid receptor family. It acts as a high-affinity antagonist with a Ki of 0.013 nM in CHO-DG44 cells expressing the mouse receptor. The compound is selective for δ2-opioid receptors over κ- and μ-opioid receptors, with Kis of 13 and 12 nM for κ and μ receptors, respectively. Naltriben mesylate also activates TRPM7 (transient receptor potential melastatin 7) channels. By blocking δ2-opioid receptors, the compound modulates opioid signaling pathways, which are involved in pain, reward, and addiction. Its TRPM7 activating activity may contribute to additional physiological effects.
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| ln Vitro |
In vitro, Naltriben mesylate potently inhibits δ2-opioid receptor-mediated signaling in cell-based assays. In CHO-DG44 cells expressing the mouse δ2-opioid receptor, the compound exhibits a Ki of 0.013 nM. It is selective for δ2 over μ and κ receptors. The compound's antagonistic activity is typically assessed by measuring inhibition of agonist-stimulated cAMP accumulation, calcium mobilization, or GTPγS binding in receptor-expressing cell lines. Naltriben mesylate also activates TRPM7 channels, an activity that is distinct from its opioid receptor antagonism. The compound is a valuable tool for studying δ2-opioid receptor function and TRPM7 channel biology.
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| ln Vivo |
Naltriben (2.5 mg/kg; subcutaneous injection; body weight 100-125 g) is a delta2 antagonist that can prevent hypothermia caused by SNC-80 (35 mg/kg; intramuscular injection) [2].
In vivo, Naltriben mesylate has been used to study the role of δ2-opioid receptors in pain, reward, and addiction. As a selective δ2 antagonist, it can block the effects of δ2-opioid receptor agonists in animal models. The compound has been used to investigate the involvement of δ2-opioid receptors in morphine tolerance, dependence, and reward. However, specific in vivo efficacy data are limited in the published literature. The compound's TRPM7 activating activity may also contribute to its in vivo effects. Naltriben mesylate is a research tool and has not been developed for clinical applications. |
| Enzyme Assay |
In vitro receptor binding assays for Naltriben mesylate typically involve competition binding studies using radiolabeled opioid receptor ligands. A typical protocol: membrane preparations from cells expressing δ2-, μ-, or κ-opioid receptors are incubated with [³H]-naltrindole (for δ receptors) or [³H]-DAMGO (for μ receptors) or [³H]-U-69593 (for κ receptors) and varying concentrations of Naltriben mesylate (0.001 nM to 10 μM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl₂, 0.1% BSA) for 60-90 minutes at room temperature. Non-specific binding is determined in the presence of 10 μM naloxone. Bound radioactivity is separated by rapid filtration and quantified by scintillation counting. IC₅₀ and Kᵢ values are calculated from competition curves using nonlinear regression. Each concentration is tested in triplicate, and experiments are repeated at least three times.
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| Cell Assay |
In vitro cell-based assays for Naltriben mesylate are performed using opioid receptor-expressing cell lines such as CHO-δ2, CHO-μ, or CHO-κ cells. A typical protocol: cells are seeded in 96-well plates at 20,000-50,000 cells/well and cultured overnight. Cells are pre-incubated with Naltriben mesylate at concentrations ranging from 0.001 nM to 10 μM for 30 minutes. Cells are then stimulated with a δ2-opioid receptor agonist (e.g., deltorphin II) for 15-30 minutes. Signaling readouts include cAMP accumulation (measured by ELISA or HTRF), calcium mobilization (measured using Fluo-4 or Fura-2 AM), or GTPγS binding (measured by scintillation proximity assay). Antagonistic activity is expressed as the percent inhibition of agonist-stimulated signaling. Each condition is tested in triplicate, and experiments are repeated at least three times.
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| Animal Protocol |
In vivo animal studies for Naltriben mesylate are conducted in rodent models of pain, reward, and addiction. A typical protocol: male Sprague-Dawley rats or C57BL/6 mice are administered Naltriben mesylate via intraperitoneal or intracerebroventricular injection at doses of 0.1-10 mg/kg. For pain studies, analgesic effects are assessed using the hot plate test or tail flick test. For reward studies, conditioned place preference or self-administration paradigms are used. The compound is typically administered 15-30 minutes before behavioral testing. Efficacy is assessed by comparing behavioral responses between treatment and vehicle control groups. The compound's effects on δ2-opioid receptor-mediated behaviors are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Naltriben mesylate have not been fully characterized. The compound is soluble in DMSO. Its plasma half-life, volume of distribution, protein binding, oral bioavailability, and clearance remain unknown. The compound is a research-grade chemical and has not been developed for clinical applications. It is primarily used for in vitro and in vivo studies of opioid receptor pharmacology. The compound should be stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for Naltriben mesylate are limited. As a research chemical, it has not undergone formal toxicology testing. Standard laboratory safety precautions should be followed when handling Naltriben mesylate: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound should be stored at -20°C for long-term stability. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling.
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| References |
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| Additional Infomation |
Additional information for Naltriben mesylate: The compound has a CAS number of 122517-78-6. Its molecular formula is C₂₇H₂₉NO₇S and molecular weight is 511.59 g/mol. Synonyms include NTB. It is a selective, high-affinity antagonist for the δ2-opioid receptor. It is a benzofuran derivative of naltrindole. Ki values: 0.013 nM for δ2, 19 nM for μ, 152 nM for κ. It is also a TRPM7 activator. Purity is typically ≥98% by HPLC. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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| Molecular Formula |
C27H29NO7S
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| Molecular Weight |
511.586666822433
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| Exact Mass |
511.166
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| CAS # |
122517-78-6
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| Related CAS # |
Naltriben;111555-58-9
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| PubChem CID |
45073482
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| Appearance |
White to off-white solid powder
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| LogP |
4.36
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
36
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| Complexity |
865
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CS(=O)(=O)O.C1CC1CN2CC[C@]34[C@@H]5C6=C(C[C@]3(C2CC7=C4C(=C(C=C7)O)O5)O)C8=CC=CC=C8O6
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| InChi Key |
XRRFZOCDAWPIBB-XXCZMEBESA-N
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| InChi Code |
InChI=1S/C26H25NO4.CH4O3S/c28-18-8-7-15-11-20-26(29)12-17-16-3-1-2-4-19(16)30-22(17)24-25(26,21(15)23(18)31-24)9-10-27(20)13-14-5-6-14;1-5(2,3)4/h1-4,7-8,14,20,24,28-29H,5-6,9-13H2;1H3,(H,2,3,4)/t20?,24-,25-,26+;/m0./s1
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| Chemical Name |
(1S,2S,13R)-22-(cyclopropylmethyl)-11,14-dioxa-22-azaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15,17,19(25)-heptaene-2,16-diol;methanesulfonic 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, avoid exposure to moisture. |
| 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) |
DMSO : ~50 mg/mL (~97.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9547 mL | 9.7735 mL | 19.5469 mL | |
| 5 mM | 0.3909 mL | 1.9547 mL | 3.9094 mL | |
| 10 mM | 0.1955 mL | 0.9773 mL | 1.9547 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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