Tianeptine sodium salt

Name: Tianeptine sodium salt
Brand: MedChemExpress
SKU: HY-90003A
Rating: 4.5 (1 reviews)

Cat. No.: HY-90003A Purity: 99.90%: Data Sheet
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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.

Tianeptine sodium salt Chemical Structure

CAS No. : 30123-17-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tianeptine sodium salt:

Tianeptine In-stock
Tianeptine sodium salt (Standard) Get quote

1 Publications Citing Use of MCE Tianeptine sodium salt

•Nat Commun. 2018 Oct 15;9(1):4272. [Abstract]

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•Related Small Molecules:

•Related Proteins:

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

IC₅₀ & Target^[2]^[5]

μ Opioid Receptor/MOR

δ Opioid Receptor/DOR

MMP-9

PI3K

NF-κB

Akt

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	14.1 μM Compound: Tianeptinum	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	[PMID: 20966043]
HepG2	EC₅₀	22.4 μM Compound: Tianeptinum	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	[PMID: 20966043]

In Vitro

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.

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) sodium salt 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 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.

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

458.93

Formula

C₂₁H₂₄ClN₂NaO₄S

CAS No.

30123-17-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(CCCCCCNC(C1=CC=CC=C1N2C)C3=CC=C(C=C3S2(=O)=O)Cl)O[Na]

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 : 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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1790 mL	10.8949 mL	21.7898 mL
5 mM	0.4358 mL	2.1790 mL	4.3580 mL
10 mM	0.2179 mL	1.0895 mL	2.1790 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.

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (287 KB) SDS (393 KB)

COA (253 KB) LCMS (93 KB)

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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.