Tianeptine sodium salt
Based on 1 publication(s) in Google Scholar
Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 30123-17-2
- Formula: C21H24ClN2NaO4S
- Molecular Weight:458.93
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tianeptine sodium salt
MoreAll Opioid Receptor Isoforms
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Biological Activity
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μ Opioid Receptor/MOR |
δ Opioid Receptor/DOR |
MMP-9 |
PI3K |
NF-κB |
Akt |
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Cell Line
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Type | Value | Description | References |
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| HepG2 | EC50 |
14.1 μM
Compound: Tianeptinum
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
22.4 μM
Compound: Tianeptinum
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
Tianeptine sodium salt inhibits the polarization of microglia/macrophages to a pro-inflammatory (M1) phenotype by stimulating MOR, and increases the activity of antioxidant enzymes such as superoxide dismutase (SOD) and catalase, thereby alleviating oxidative stress damage[2].
Tianeptine sodium salt can increase BDNF and NGF levels in brain regions such as the hippocampus and amygdala, and promote neurogenesis in the dentate gyrus of the hippocampus[2].
Tianeptine (0.1-100 μM, 14 days) sodium salt significantly reduces hypoxia-induced LDH release in rat embryonic cortical neurons[4].
Tianeptine (10 μM) sodium salt does not reduce neuronal apoptosis induced directly by NMDA (HY-17551), but shows a slight but significant protective effect in the presence of IL-1β in mouse cortical neurons[4].
Tianeptine sodium salt demonstrates low cardiotoxicity and minimal risk of CYP-mediated drug-drug interactions (DDIs)[1].
Tianeptine sodium salt (125-500 µM, 24 h) suppresses TNF-α-induced expression of MMP-9 in human carcinoma cells MDA-MB-231 via suppression of the PI3K/Akt-mediated NF-κB pathway[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells
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Concentration:500 μM
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Incubation Time:24 h
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Result:Significantly attenuated TNF-α-stimulated cancer cell invasion.
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Cell Line:LNCaP cells
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Concentration:125, 250, 500 μM
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Incubation Time:1, 6 h
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Result:Dose-dependent inhibited MMP-9 expression.
Blocked TNF-α-induced IκBα degradation and p65/p50 nuclear translocation.
Inhibited TNF-α-induced phosphorylation of PI3K and Akt.
Tianeptine sodium salt does not modify the rate of extracellular serotonin in rats, so it does not increase or decrease the reuptake of serotonin[2].
Tianeptine sodium salt improves cognitive deficits and memory impairment caused by stress, and enhances learning ability and spatial memory[2].
Tianeptine (5-10 mg/kg, i.p., single dose) sodium salt exhibits significant analgesic effects in both the hot-plate and tail-flick thermal pain models in mice without causing motor impairment[3].
Tianeptine (1-10 mg/kg, i.p., single dose or twice daily for 5 days) sodium salt shows neuroprotective effect which is not achieved by directly antagonizing NMDA receptors, but is only fully stimulated in pathological conditions with inflammatory/cytokine provocation[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Corticosterone release assay established in male Wistar rats, weighing initially 260-280 g[1]
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Dosage:10 mg/kg (without Benserazide (HY-121275)) and 50 mg/kg (with Benserazide)
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Did not antagonize 5-HTP-induced peripheral corticosterone release. Specifically antagonized the appetite suppression and weight loss effects caused by increased central 5-HT.
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Animal Model:Hot-plate and tail-flick model established in adult male Swiss Webster mice (25-32 g)[3]
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Dosage:5 and 10 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Significantly prolonged the latency of pain response in both the tail-flick and hot plate tests, demonstrating a strong analgesic effect at 10 mg/kg. Completely blocked the analgesic effect in both pain models pretreatment with pCPA (HY-B1368). Did not affect the performance of mice on the rotating rod.
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Animal Model:Model of cerebral cortex and white matter area damage established in Newborn Swiss mice on postnatal day 5 (P5)[4]
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Dosage:1, 3 and 10 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose or twice daily for 5 days
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Result:Failed to alleviate the underlying impairment caused by ibotenate with acute or chronic administration. Effectively reversed damage exacerbated by chronic IL-1β pretreatment.
Chemical Information
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CAS No. 30123-17-2
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Appearance Solid
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Molecular Weight 458.93
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Formula C21H24ClN2NaO4S
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Color White to off-white
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SMILES
O=C(CCCCCCNC(C1=CC=CC=C1N2C)C3=CC=C(C=C3S2(=O)=O)Cl)O[Na]
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Modulation of AMPA receptor surface diffusion restores hippocampal plasticity and memory in Huntington's disease models. [Abstract]2018 Oct 15;9(1):4272. PMID: 30323233
Solvent & Solubility
DMSO : 100 mg/mL (217.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (217.90 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.45 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.45 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 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (287 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Broqua P; Baudrie V; Chaouloff F Differential effects of the novel antidepressant tianeptine on L-5-hydroxytryptophan (5-HTP)-elicited corticosterone release and body weight loss. Eur Neuropsychopharmacol. 1992 Jun;2(2):115-20. [Content Brief]
[2]. Alamo C, et, al. Tianeptine, an atypical pharmacological approach to depression. Rev Psiquiatr Salud Ment. Jul-Sep 2019;12(3):170-186. [Content Brief]
[3]. Uzbay IT, et, al. Analgesic effect of tianeptine in mice. Life Sci. 1999;64(15):1313-9. [Content Brief]
[4]. Plaisant F, et, al. Neuroprotective properties of tianeptine: interactions with cytokines. Neuropharmacology. 2003 May;44(6):801-9. [Content Brief]
[5]. Jayasooriya RG, et al. Tianeptine sodium salt suppresses TNF-α-induced expression of matrix metalloproteinase-9 in human carcinoma cells via suppression of the PI3K/Akt-mediated NF-κB pathway. Environ Toxicol Pharmacol. 2014 Sep;38(2):502-9. [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 |
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| DMSO / H2O | 1 mM | 2.1790 mL | 10.8949 mL | 21.7898 mL | 54.4745 mL |
| 5 mM | 0.4358 mL | 2.1790 mL | 4.3580 mL | 10.8949 mL | |
| 10 mM | 0.2179 mL | 1.0895 mL | 2.1790 mL | 5.4475 mL | |
| 15 mM | 0.1453 mL | 0.7263 mL | 1.4527 mL | 3.6316 mL | |
| 20 mM | 0.1089 mL | 0.5447 mL | 1.0895 mL | 2.7237 mL | |
| 25 mM | 0.0872 mL | 0.4358 mL | 0.8716 mL | 2.1790 mL | |
| 30 mM | 0.0726 mL | 0.3632 mL | 0.7263 mL | 1.8158 mL | |
| 40 mM | 0.0545 mL | 0.2724 mL | 0.5447 mL | 1.3619 mL | |
| 50 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0895 mL | |
| 60 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9079 mL | |
| 80 mM | 0.0272 mL | 0.1362 mL | 0.2724 mL | 0.6809 mL | |
| 100 mM | 0.0218 mL | 0.1089 mL | 0.2179 mL | 0.5447 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Tianeptine sodium salt Related Classifications
HY-90003A Related Classifications
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