For research use only.
Catalog No.S1259 Synonyms: TAK-375
CAS No. 196597-26-9
Ramelteon (TAK-375) 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.
Selleck's Ramelteon has been cited by 7 publications
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(M) (Left) Cresyl violet and Luxol fast blue staining of ipsilateral corpus striatum on day 3 post-TBI. Scale bar = 50 µm. (Right) Bar graph shows that ramelteon did not increase the percentage of area with normal myelin in the Nrf2 KO mouse brain compared with that in the vehicle group. n = 6 mice/group. *P < 0.05 vs. sham group (one-way ANOVA followed by Bonferroni post hoc test). (N) (Left) Fluoro-Jade C staining of the perilesional cerebral cortex on day 3 post-TBI. Scale bar = 30 µm. (Right) Bar graph shows that ramelteon did not decrease the number of degenerating neurons in the perilesional region of the Nrf2 KO mice. n = 6 mice/group. *P < 0.05 vs. sham group (one-way ANOVA followed by Bonferroni post hoc test).
Free Radic Biol Med, 2018, 131:345-355. Ramelteon purchased from Selleck.
(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.
Porphyromonas gingivalis were incubated in the presence of ramelteon (B). After crystal violet staining, absorbance at 550 nm was recorded. Data represent the mean ± SEM (n = 3) and differences between groups were assessed by ANOVA, *P < 0.05 versus vehicle control; **P < 0.01 versus vehicle control. three experiments.
PLoS One, 2016, 11(11):e0166442. Ramelteon purchased from Selleck.
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Choose Selective MT Receptor Inhibitors
|Description||Ramelteon (TAK-375) 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.|
Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells.  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.  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. 
|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.  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.  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. |
-  Kato K, et al. Neuropharmacology, 2005, 48(2), 301-310.
-  Fisher SP, et al. J Pineal Res, 2008, 45(2), 125-132.
-  Imbesi M, et al. Neuroscience, 2008, 155(4), 1160-1164.
|In vitro||DMSO||52 mg/mL (200.5 mM)|
|Ethanol||52 mg/mL (200.5 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
1.Please make sure the liquid is clear before adding the next solvent.
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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03931070||Unknown status||Drug: Ramelteon|Drug: Placebo - Cap||Delirium||Rhode Island Hospital||May 9 2019||Phase 4|
|NCT02560324||Completed||Drug: Ramelteon|Drug: Placebo||Tobacco Use Disorder||University of Pennsylvania|National Institute on Drug Abuse (NIDA)|National Institutes of Health (NIH)||September 2015||Phase 2|
|NCT02969343||Completed||Behavioral: Patient Safety health information technology||Central Line-Associated Bloodstream Infection (CLABSI)|Venous Thromboembolism|Patient Fall|Catheter-Associated Infection|Severe Hypoglycemia|Opioid-Related Severe Adverse Drug Event|Hospital Acquired Pressure Ulcer|Adverse Drug Event|Severe Hospital Acquired Delerium|Rapid Response Related to Arrhythmia||Brigham and Women''s Hospital|Northeastern University||April 2015||Not Applicable|
|NCT00568789||Completed||Drug: Ramelteon zolpidem and placebo||Insomnia||Takeda||June 2006||Phase 4|
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.
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