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Agomelatine (S20098)

Name: Agomelatine (S20098)
Brand: Selleck Chemicals
SKU: S1243
Rating: 5 (4 reviews)

Synonyms: Valdoxan, Melitor, Thymanax,S20098

Catalog No.S1243 Purity: 99.89%

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

CAS: 138112-76-2

Selleck's Agomelatine (S20098) has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.89%

99.89

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Cell Data

Cell Lines	Assay Type	Incubation Time	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
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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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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

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