2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Metabolic Enzyme/Protease PI3K/Akt/mTOR NF-κB
  3. Opioid Receptor iGluR MMP PI3K Akt NF-κB
  4. Tianeptine

Tianeptine is an atypical antidepressant. Tianeptine 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 is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine 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.

Tianeptine

Tianeptine Chemical Structure

CAS No. : 72797-41-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tianeptine:

Tianeptine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tianeptine

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

View All iGluR Isoform Specific Products:

View All Isoforms
AMPA Receptor NMDA Receptor Kainate Receptor

View All MMP Isoform Specific Products:

View All Isoforms
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tianeptine is an atypical antidepressant. Tianeptine 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 is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects[1][2][3][4][5].

IC50 & Target[2][5]

μ Opioid Receptor/MOR

 

δ Opioid Receptor/DOR

 

MMP-9

 

Akt

 

PI3K

 

NF-κB

 

In Vitro

Tianeptine 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 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) significantly reduces hypoxia-induced LDH release in rat embryonic cortical neurons[4].
Tianeptine (10 μM) 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 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.

Tianeptine Related Antibodies

Cell Invasion Assay[5]

Cell Line: LNCaP cells
Concentration: 500 μM
Incubation Time: 24 h
Result: Significantly attenuated TNF-α-stimulated cancer cell invasion.

Western Blot Analysis[5]

Cell Line: LNCaP cells
Concentration: 125, 250, 500 μM
Incubation Time: 1, 6 h
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.
In Vivo

Tianeptine (10 and 50 mg/kg, i.p., single dose) selectively antagonizes the physiological and behavioral effects (weight loss) induced by increased central 5-HT, but does not affect the effects (corticosterone release) induced by increased peripheral 5-HT[1].
Tianeptine does not modify the rate of extracellular serotonin in rats, so it does not increase or decrease the reuptake of serotonin[2].
Tianeptine 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) 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) 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.

Animal Model: Corticosterone release assay established in male Wistar rats, weighing initially 260-280 g[1]
Dosage: 10 mg/kg (without Benserazide (HY-121275)) and 50 mg/kg (with Benserazide)
Administration: Intraperitoneal injection (i.p.), single dose
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.
Animal Model: Hot-plate and tail-flick model established in adult male Swiss Webster mice (25-32 g)[3]
Dosage: 5 and 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
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.
Animal Model: Model of cerebral cortex and white matter area damage established in Newborn Swiss mice on postnatal day 5 (P5)[4]
Dosage: 1, 3 and 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose or twice daily for 5 days
Result: Failed to alleviate the underlying impairment caused by ibotenate with acute or chronic administration.
Effectively reversed damage exacerbated by chronic IL-1β pretreatment.
Clinical Trial
Molecular Weight

436.95

Formula

C21H25ClN2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CCCCCCNC(C1=CC=CC=C1N2C)C3=CC=C(C=C3S2(=O)=O)Cl)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (22.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2886 mL 11.4430 mL 22.8859 mL
5 mM 0.4577 mL 2.2886 mL 4.5772 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (2.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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 2.2886 mL 11.4430 mL 22.8859 mL 57.2148 mL
5 mM 0.4577 mL 2.2886 mL 4.5772 mL 11.4430 mL
10 mM 0.2289 mL 1.1443 mL 2.2886 mL 5.7215 mL
15 mM 0.1526 mL 0.7629 mL 1.5257 mL 3.8143 mL
20 mM 0.1144 mL 0.5721 mL 1.1443 mL 2.8607 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Tianeptine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tianeptine72797-41-2Opioid ReceptoriGluRMMPPI3KAktNF-κBIonotropic glutamate receptorsMatrix metalloproteinasesPhosphoinositide 3-kinasePKBProtein kinase BNuclear factor-κBNuclear factor-kappaBanalgesiaantidepressantserotoninmiceInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tianeptine
Cat. No.:
HY-90003
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.