Naltrexone
Based on 1 Customer Validation
Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 16590-41-3
- Formula: C20H23NO4
- Molecular Weight:341.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Opioid Receptor Isoforms
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Biological Activity
|
μ Opioid Receptor/MOR |
κ Opioid Receptor/KOR |
δ Opioid Receptor/DOR |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BV-2 | IC50 |
105.5 μM
Compound: 31
|
Inhibition of LPS-induced NO production in mouse BV-2 microglia cells incubated for 24 hrs by 2,3-diaminonaphthalene assay
Inhibition of LPS-induced NO production in mouse BV-2 microglia cells incubated for 24 hrs by 2,3-diaminonaphthalene assay
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[PMID: 35307617] |
| CHO | EC50 |
0.16 nM
Compound: NTX
|
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
|
[PMID: 23948248] |
| CHO | EC50 |
0.16 nM
Compound: NTX
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Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
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[PMID: 25783191] |
| CHO | EC50 |
0.38 nM
Compound: NTX
|
Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
Agonist activity at mu opioid receptor (unknown origin) expressed CHO cells assessed as stimulation of [35S]-GTP[gammaS] binding
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[PMID: 23721804] |
| CHO | EC50 |
0.59 Ke/nM
Compound: NTX (1)
|
Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells
Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells
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[PMID: 12672258] |
| CHO | EC50 |
0.81 nM
Compound: NTX
|
Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
|
[PMID: 24144240] |
| CHO | EC50 |
0.81 nM
Compound: NTX
|
Agonist activity at mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
Agonist activity at mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
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[PMID: 25783191] |
| CHO | EC50 |
1.86 Ke/nM
Compound: NTX (1)
|
Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.
Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.
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[PMID: 12672258] |
| CHO | EC50 |
16 nM
Compound: 3, NTRX
|
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
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[PMID: 19282177] |
| CHO | EC50 |
21 nM
Compound: 3, NTRX
|
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | EC50 |
3.3 nM
Compound: 3, NTRX
|
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | EC50 |
4.4 nM
Compound: NTX
|
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs
|
[PMID: 24144240] |
| CHO | EC50 |
4.4 nM
Compound: NTX
|
Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
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[PMID: 25783191] |
| CHO | EC50 |
5.44 nM
Compound: NTX
|
Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay
|
[PMID: 24973818] |
| CHO | EC50 |
5.44 Ke/nM
Compound: NTX (1)
|
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
|
[PMID: 12672258] |
| CHO | IC50 |
0.59 nM
Compound: 3d
|
Activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
Activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
|
[PMID: 17004724] |
| CHO | IC50 |
0.95 nM
Compound: NTX
|
Binding affinity to MOR Y210A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay
Binding affinity to MOR Y210A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay
|
[PMID: 24055076] |
| CHO | IC50 |
1.86 nM
Compound: 3d
|
Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
Activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
|
[PMID: 17004724] |
| CHO | IC50 |
10.35 nM
Compound: NTX
|
Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay
Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay
|
[PMID: 24055076] |
| CHO | IC50 |
130 nM
Compound: 3, NTRX
|
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
Antagonist activity against human delta opioid receptor expressed in CHO cells assessed as inhibition of SNC80-stimulated [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | IC50 |
130 nM
Compound: 3, NTRX
|
Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-stimulated [35S]GTPgammaS binding
Antagonist activity against human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-stimulated [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | IC50 |
15.5 nM
Compound: NTX
|
Antagonist activity at human MOR expressed in CHO cells assessed as inhibition of DAMGO-induced increase in intracellular Ca2+ level incubated for 15 mins prior to DAMGO addition by microplate reader analysis
Antagonist activity at human MOR expressed in CHO cells assessed as inhibition of DAMGO-induced increase in intracellular Ca2+ level incubated for 15 mins prior to DAMGO addition by microplate reader analysis
|
[PMID: 25783191] |
| CHO | IC50 |
17 nM
Compound: 3
|
Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as inhibition of DAGO-stimulated [35S]GTPgammaS binding
Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as inhibition of DAGO-stimulated [35S]GTPgammaS binding
|
[PMID: 17407276] |
| CHO | IC50 |
200 nM
Compound: 3
|
Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U-50488-stimulated [35S]GTP-gamma-S binding
Antagonist activity at human opioid kappa receptor expressed in CHO cells assessed as inhibition of U-50488-stimulated [35S]GTP-gamma-S binding
|
[PMID: 17407276] |
| CHO | IC50 |
3.9 nM
Compound: NTX
|
Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay
Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay
|
[PMID: 24055076] |
| CHO | IC50 |
4.1 nM
Compound: 1b
|
Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells
Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells
|
[PMID: 17149859] |
| CHO | IC50 |
4.1 nM
Compound: 2b
|
Antagonist activity against human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding
Antagonist activity against human cloned mu opioid receptor expressed in CHO cells assessed as inhibition of loperamide-stimulated [35S]GTP-gamma-S binding
|
[PMID: 17149858] |
| CHO | IC50 |
4.8 nM
Compound: 3, NTRX
|
Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding
Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding
|
[PMID: 19282177] |
| CHO | IC50 |
5.44 nM
Compound: 3d
|
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
Activity at human recombinant delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
|
[PMID: 17004724] |
| CHO | IC50 |
8.9 nM
Compound: NTX
|
Antagonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells assessed as inhibition of DAMGO-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge
Antagonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells assessed as inhibition of DAMGO-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge
|
[PMID: 23682308] |
| HEK293 | IC50 |
157.51 μM
Compound: Naltrexone
|
Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis
Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis
|
[PMID: 31597043] |
Naltrexone (1-100 μM; 48-120 h) inhibited proliferation of SKOV-3, MDA-MB-231, SK-N-MC, OVCAR-3, MIA PaCa-2, SCC-1, and HCT-116 cancer cells via intermittent or short-term treatment, while continuous treatment stimulated proliferation[3].
Naltrexone (1.0 mg/mL; 24-72 h) inhibited proliferation of SW480 and HCT116 colon cancer cells in a time-dependent manner, with maximum inhibition at 72 h[3].
Naltrexone (1 μM) increases the activity of mouse hypothalamic arcuate POMC-EGFP cells in vitro, and this effect is amplified when combined with Bupropion[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV-3 human ovarian cancer cells, MDA-MB-231 triple negative breast cancer cells, SK-N-MC human neuroblastoma cells, OVCAR-3 human ovarian carcinoma cells, MIA PaCa-2 human pancreatic carcinoma cells, SCC-1 human squamous carcinoma cells, HCT-116 human colon carcinoma cells
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Concentration:1, 10 and 100 μM
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Incubation Time:48, 72, 96 and 120 h
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Result:Reduced SKOV-3 cell numbers by 42% (10 μM, 120 h intermittent).
Reduced MDA-MB-231 cell numbers by 35% (1 μM, 72 h intermittent).
Reduced SK-N-MC cell numbers by 35% (100 μM, 48 h continuous).
Reduced SKOV-3 cell numbers by 29% (10 μM, 96 h short-term).
Reduced SKOV-3 cell numbers by 32% (10 μM, 72 h short-term).
Reduced OVCAR-3 cell numbers by 28% (10 μM, 72 h short-term).
Reduced MIA PaCa-2 cell numbers by 31% (10 μM, 72 h short-term).
Reduced SCC-1 cell numbers by 26% (10 μM, 72 h short-term).
Reduced HCT-116 cell numbers by 24% (10 μM, 72 h short-term).
Increased cell numbers in multiple cell lines with continuous treatment.
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Cell Line:SW480 human colon cancer cells, HCT116 human colon cancer cells
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Concentration:1.0 mg/mL
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Incubation Time:24 h, 48 h, 72 h
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Result:Inhibited SW480 cell proliferation by 6% (24 h), 23% (48 h), and 41% (72 h).
Inhibited HCT116 cell proliferation by 16% (24 h), 45% (48 h), and 68% (72 h) relative to control.
Naltrexone (0.1 mg/kg; i.p.; daily administration; for 40 consecutive days) reduces the number and weight of tumor nodules in mice bearing SKOV-3 human epithelial ovarian cancer[3].
Naltrexone (1-75 mg/kg; administered via dietary supplementation or injection; dosing frequency of twice weekly or twice daily; treatment duration of 25 days) reduces the tumor volume and diameter in DMBA (HY-W011845)-induced breast cancer rats, and a higher dose of the injection route results in a greater reduction in tumor diameter[3].
Naltrexone (0.1-10 mg/kg; intravenous injection; once daily; for 75 consecutive days) at low-dose administration extend the survival time of mice in the S20Y mouse neuroblastoma model, while high doses increase tumor diameter, shorten the latency period, and reduce survival time in this mouse model[3].
Naltrexone (0.1 mg/kg; intravenous injection; once daily; for 50 consecutive days) reduces tumor incidence and prolongs the latency period in mice bearing HT-29 human colon cancer[3].
Naltrexone reduces food intake in diet-induced obesity (DIO) mice and fasted lean mice, and exerts a synergistic effect when combined with Bupropion[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 16590-41-3
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Appearance Solid
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Molecular Weight 341.40
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Formula C20H23NO4
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Color White to off-white
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SMILES
OC1=CC=C2C3=C1O[C@](C(CC4)=O)([H])[C@@]3(CCN5CC6CC6)[C@]4(O)[C@@]5([H])C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (292.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.65 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (288 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lee B, et al. The uses of naltrexone in dermatologic conditions. J Am Acad Dermatol. 2019;80(6):1746-1752. [Content Brief]
[2]. Younger J, et al. The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain. Clin Rheumatol. 2014;33(4):451-459. [Content Brief]
[3]. Liubchenko K, et al. Naltrexone's Impact on Cancer Progression and Mortality: A Systematic Review of Studies in Humans, Animal Models, and Cell Cultures. Adv Ther. 2021;38(2):904-924. [Content Brief]
[4]. Lobmaier PP, et al. Naltrexone depot formulations for opioid and alcohol dependence: a systematic review. CNS Neurosci Ther. 2011;17(6):629-636. [Content Brief]
[5]. Billes SK, et al. Naltrexone/bupropion for obesity: an investigational combination pharmacotherapy for weight loss. Pharmacol Res. 2014;84:1-11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9291 mL | 14.6456 mL | 29.2912 mL | 73.2279 mL |
| 5 mM | 0.5858 mL | 2.9291 mL | 5.8582 mL | 14.6456 mL | |
| 10 mM | 0.2929 mL | 1.4646 mL | 2.9291 mL | 7.3228 mL | |
| 15 mM | 0.1953 mL | 0.9764 mL | 1.9527 mL | 4.8819 mL | |
| 20 mM | 0.1465 mL | 0.7323 mL | 1.4646 mL | 3.6614 mL | |
| 25 mM | 0.1172 mL | 0.5858 mL | 1.1716 mL | 2.9291 mL | |
| 30 mM | 0.0976 mL | 0.4882 mL | 0.9764 mL | 2.4409 mL | |
| 40 mM | 0.0732 mL | 0.3661 mL | 0.7323 mL | 1.8307 mL | |
| 50 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL | 1.4646 mL | |
| 60 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2205 mL | |
| 80 mM | 0.0366 mL | 0.1831 mL | 0.3661 mL | 0.9153 mL | |
| 100 mM | 0.0293 mL | 0.1465 mL | 0.2929 mL | 0.7323 mL |