Agomelatine (S20098)

Synonyms: Valdoxan, Melitor, Thymanax,S20098

Agomelatine (Valdoxan, Melitor, Thymanax,S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

Agomelatine (S20098) Chemical Structure

Agomelatine (S20098) Chemical Structure

CAS No. 138112-76-2

Purity & Quality Control

Agomelatine (S20098) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK 293 Function assay Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=6e-05 μM 12646022
CHO cells Function assay 120 mins Displacement of [125I]iodomelatonin form human MT1 receptor expressed in CHO cells after 120 mins, Ki=0.1 nM 22301214
CHO-Galpha16 cells Function assay 20 mins Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=2.1 nM 21237644
Click to View More Cell Line Experimental Data

Biological Activity

Description Agomelatine (Valdoxan, Melitor, Thymanax,S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.
Targets
5-HT2C [1]
In vitro
In vitro

Agomelatine completely normalizes stress-affected cell survival and partly reverses reduced doublecortin expression in the hippocampus of rats subjected to chronic footshock stress. [1]

In Vivo
In vivo

Agomelatine is effective in reversing the transgenic mouse behavioural changes noted in the Porsolt forced swim test as well as in the elevated plus maze. Agomelatine also markedly accelerates readjustment of circadian cycles of temperature and activity following an induced phase shift. [2] Agomelatine enhances cell proliferation and neurogenesis in the ventral hippocampus (VH) of adult rats, a region pertinent to mood disorders. Agomelatine increases the ratio of mature vs immature neurons and enhances neurite outgrowth of granular cells in adult rats, suggesting an acceleration of maturation. Agomelatine also activates several cellular signals (extracellular signal-regulated kinase1/2, protein kinase B, and glycogen synthase kinase 3beta) known to be modulated by antidepressants and implicated in the control of proliferation/survival. [3] Agomelatine enhances the time devoted to active social interaction in unfamiliar pairs of rats exposed to a novel environment. [4] Agomelatine increases cell proliferation and neurogenesis in the ventral dentate gyrus of rats, a region notably implicated in response to emotion, which is consistent with the antidepressant-anxiolytic properties of Agomelatine. Agomelatine increases survival of newly formed neurons in the entire dentate gyrus of rats. [5]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06120543 Not yet recruiting
Polymorphism Genetic|Depression|CYP1A2 Polymorphism|CYP2C9 Polymorphism|Polymerase Chain Reaction|Plasma Concentration
Affiliated Hospital of Nantong University
October 31 2023 --
NCT05323994 Recruiting
Depression|COVID-19
Servier Russia
April 19 2022 --
NCT03977441 Unknown status
Parkinson Disease|Depression|Sleep Disorders|Circadian Rhythm Disorders
Second Affiliated Hospital of Soochow University
July 2019 Phase 4
NCT00463242 Completed
Major Depressive Disorder
Novartis
March 2007 Phase 3

Chemical Information & Solubility

Molecular Weight 243.3 Formula

C15H17NO2

CAS No. 138112-76-2 SDF Download Agomelatine (S20098) SDF
Smiles CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 48 mg/mL ( (197.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Agomelatine (S20098) | Agomelatine (S20098) ic50 | Agomelatine (S20098) price | Agomelatine (S20098) cost | Agomelatine (S20098) solubility dmso | Agomelatine (S20098) purchase | Agomelatine (S20098) manufacturer | Agomelatine (S20098) research buy | Agomelatine (S20098) order | Agomelatine (S20098) mouse | Agomelatine (S20098) chemical structure | Agomelatine (S20098) mw | Agomelatine (S20098) molecular weight | Agomelatine (S20098) datasheet | Agomelatine (S20098) supplier | Agomelatine (S20098) in vitro | Agomelatine (S20098) cell line | Agomelatine (S20098) concentration | Agomelatine (S20098) nmr