Catalog No.S1259 Synonyms: TAK-375

Ramelteon Chemical Structure

Molecular Weight(MW): 259.34

Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.

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In DMSO USD 280 In stock
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  • (A) CLSM images of Porphyromonas gingivalis biofilm formed in the presence of melatonin and ramelteon at sub-MIC concentrations. Biofilm-forming cells were stained using the Live/Dead Bacterial Viability Kit. Dead cells were stained red, whereas live bacteria were stained green. In the presence of 50 μg/mL or 25 μg/mL ramelteon, the areas of biofilm formation were narrower than that of vehicle controls. Bars = 50 μm.

    PLoS One, 2016, 11(11):e0166442.. Ramelteon purchased from Selleck.

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Biological Activity

Description Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.
Features A tricyclic synthetic analog of melatonin.
MT1 receptor [1]
(Cell-free assay)
MT receptor (chicken) [1]
(Cell-free assay)
MT2 receptor [1]
(Cell-free assay)
14 pM(Ki) 23.1 pM(Ki) 112 pM(Ki)
In vitro

Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. [1] Ramelteon has high affinity with recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. Ramelteon inhibits Xenopus laevis melanophore pigment granule aggregation with pEC50 of 11.48. [2] Ramelteon (1 nM) increases ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells but also in cerebellar granule cells expressing only one of the two melatonin receptors. 4P-PDOT blocks the stimulatory action of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, while luzindole attenuates the action of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon (100 μM) induces any pigment dispersion while melatonin completely disperses aggregated melanophores at 10 μM. [3]

In vivo Ramelteon (10 mg/kg, i/p) significantly reduces NREM sleep latency in rat and also produces a short-lasting increase in nonrapid eye movement (NREM) sleep duration, but the NREM power spectrum is unaltered. [2] Ramelteon (0.1 mg/kg and 1 mg/kg, p.o.) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle in rats without affecting learning or memory. [4] Ramelteon (0.03 mg/kg and 0.3 mg/kg, p.o.) significantly shortens latency to sleep onset and significantly increases total duration of sleep in freely moving monkeys without affecting the general behavior of the monkeys. [5]


Animal Research:[4]
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  • Animal Models: estrogen-deficient ovariectomized (OVX) rats
  • Formulation: 0.5% methylcellulose solution
  • Dosages: 1 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 52 mg/mL (200.5 mM)
Ethanol 52 mg/mL (200.5 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
0.5% methylcellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 259.34


CAS No. 196597-26-9
Storage powder
in solvent
Synonyms TAK-375

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02669082 Not yet recruiting Insomnia|Major Depressive Disorder Takeda February 2017 Phase 4
NCT02324153 Not yet recruiting Delirium|Delirium, Dementia, Amnestic, Cognitive Disorders|Delayed Emergence From Anesthesia|Cognitive Disorders Karin J. Neufeld MD MPH|Johns Hopkins University September 2016 Phase 2
NCT02840591 Not yet recruiting Delirium University of Texas Southwestern Medical Center July 2016 Phase 4
NCT02691013 Not yet recruiting Delirium|Sleep Deprivation University of California, San Diego February 2016 --
NCT02564939 Not yet recruiting Delirium Hartford Hospital October 2015 Phase 4
NCT02560324 Recruiting Tobacco Use Disorder University of Pennsylvania|National Institute on Drug Abuse (NIDA)|National Institutes of Health (NIH) September 2015 Phase 2

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