Agomelatine (L(+)-Tartaric acid) (Synonyms: S-20098 L(+)-Tartaric acid)

Name: Agomelatine (L(+)-Tartaric acid)
Brand: MedChemExpress
SKU: HY-17038B
Rating: 5.0 (4 reviews)

Cat. No.: HY-17038B Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

For research use only. We do not sell to patients.

Agomelatine (L(+)-Tartaric acid) Chemical Structure

CAS No. : 824393-18-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 312	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 396	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 4 publication(s) in Google Scholar

Other Forms of Agomelatine (L(+)-Tartaric acid):

Agomelatine In-stock
Agomelatine hydrochloride In-stock

4 Publications Citing Use of MCE Agomelatine (L(+)-Tartaric acid)

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MT1 MT2

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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively^[1]. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively^[2].

IC₅₀ & Target

5-HT_2C Receptor

6.4 (pKi, native porcine)

5-HT_2C Receptor

6.2 (pKi, human)

hMT1

0.1 nM (Ki, CHO Cells)

hMT1

0.06 nM (Ki, HEK Cells)

hMT2

0.12 nM (Ki, CHO Cells)

hMT2

0.27 nM (Ki, HEK Cells)

In Vitro

Agomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC₅₀s of 1.6±0.4, 0.10±0.04 nM for CHO hMT1 CHO-hMT2 (hΜΤ1 and hΜΤ2 receptors expressed in CHO or HEK cell membranes)^[1].
Agomelatine (S20098) also interacts with h5-HT2B receptors (6.6), whereas it shows low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors, and negligible (<5.0) affinity for other 5-HT receptors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Swiss mice (20-30 g) were administered PTZ (85 mg/kg, i.p.), PTX (7 mg/kg, i.p.), strychnine (75 mg/kg, i.p.), Pilocarpine (400 mg/kg, i.p.), respectively^[3]
Dosage:	25, 50, or 75 mg/kg
Administration:	Administered intraperitoneally (i.p.)
Result:	All dosages showed a significant decrease in thiobarbituric acid reactive substances (TBARS) levels and nitrite content in all brain areas when compared to controls in the Pilocarpine induced seizure model. All dosages decreased TBARS levels in all brain areas, and at low doses (25 or 50 mg/kg) decreased nitrite contents, but only at 25 or 50 mg/kg showed a significant increase in catalase activity in three brain areas when compared to controls in the Strychnine-induced seizure model. Did not have any antioxidant effects on parameters of oxidative stress produced by PTX- or PTZ-induced seizure models when compared to controls.

Clinical Trial

Molecular Weight

393.39

Formula

C₁₉H₂₃NO₈

CAS No.

824393-18-2

Appearance

Solid

Color

White to off-white

SMILES

CC(NCCC1=C2C=C(OC)C=CC2=CC=C1)=O.O=C(O)[C@H](O)[C@@H](O)C(O)=O

Structure Classification

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (254.20 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	2.5420 mL	12.7100 mL	25.4201 mL
5 mM	0.5084 mL	2.5420 mL	5.0840 mL
10 mM	0.2542 mL	1.2710 mL	2.5420 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 (sealed storage, away from moisture). 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)

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 (6.36 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (6.36 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 (6.36 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.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 99.82%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (252 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

[1]. Audinot V, et al. New selective ligands of human cloned melatonin MT1 and MT2 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jun;367(6):553-61. [Content Brief]

[2]. Millan MJ, et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. J Pharmacol Exp Ther. 2003 Sep;306(3):954-64. [Content Brief]

[3]. Aguiar CC, et al. Effects of agomelatine on oxidative stress in the brain of mice after chemically induced seizures. Cell Mol Neurobiol. 2013 Aug;33(6):825-35. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5420 mL	12.7100 mL	25.4201 mL	63.5502 mL
	5 mM	0.5084 mL	2.5420 mL	5.0840 mL	12.7100 mL
	10 mM	0.2542 mL	1.2710 mL	2.5420 mL	6.3550 mL
	15 mM	0.1695 mL	0.8473 mL	1.6947 mL	4.2367 mL
	20 mM	0.1271 mL	0.6355 mL	1.2710 mL	3.1775 mL
	25 mM	0.1017 mL	0.5084 mL	1.0168 mL	2.5420 mL
	30 mM	0.0847 mL	0.4237 mL	0.8473 mL	2.1183 mL
	40 mM	0.0636 mL	0.3178 mL	0.6355 mL	1.5888 mL
	50 mM	0.0508 mL	0.2542 mL	0.5084 mL	1.2710 mL
	60 mM	0.0424 mL	0.2118 mL	0.4237 mL	1.0592 mL
	80 mM	0.0318 mL	0.1589 mL	0.3178 mL	0.7944 mL
	100 mM	0.0254 mL	0.1271 mL	0.2542 mL	0.6355 mL

Agomelatine (L(+)-Tartaric acid) Related Classifications

Neurological Disease

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:

Agomelatine (L(+)-Tartaric acid)824393-18-2S-20098 L(+)-Tartaric acidMelatonin Receptor5-HT ReceptorEndogenous MetaboliteSerotonin Receptor5-hydroxytryptamine ReceptorMT1MT2Agonist5-HT2CAntagonistdepressivedisorderantidepressantInhibitorinhibitorinhibit

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Agomelatine (L(+)-Tartaric acid) (Synonyms: S-20098 L(+)-Tartaric acid)

Customer Review

Other Forms of Agomelatine (L(+)-Tartaric acid):

Agomelatine (L(+)-Tartaric acid) Related Antibodies

4 Publications Citing Use of MCE Agomelatine (L(+)-Tartaric acid)

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Melatonin Receptor Isoform Specific Products:

View All 5-HT Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Agomelatine (L(+)-Tartaric acid) Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Agomelatine (L(+)-Tartaric acid) Related Classifications

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