Ramelteon (Synonyms: TAK-375) |
| Catalog No.GC15053 |
Ramelteon est un agoniste puissant, hautement sélectif et actif par voie orale de MT1/MT2 avec des valeurs de Ki de 14 et 112 pM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 196597-26-9
Sample solution is provided at 25 µL, 10mM.
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Ramelteon, a chronohypnotic, is an orally active and highly selective melatonin receptor (MT1, MT2 and MT3) agonist that preferentially binds to MT1 and MT2 receptors leading to potent inhibition of cAMP production in human cells expressing MT1 or MT2 receptors with the half maximal inhibition concentration IC50 values of 21.2 pM/L and 53.4 pM/L respectively [1].
The s-configuration and ether group in the chemical structure of ramelteon confer its high affinity towards MT1 and MT2 receptors with the dissociation constant Ki values of 14 pM and 112 pM respectively in comparison with that of 2650 nM for MT3 receptors [1].
Ramelteon has been found to potently promote sleep without causing any significant adverse effects leading to its application for the treatment of insomnia [1].
References:
[1] Miyamoto M. Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders. CNS Neurosci Ther. 2009 Winter;15(1):32-51. doi: 10.1111/j.1755-5949.2008.00066.x.
| Kinase experiment [1]: | |
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Binding assays |
Cells stably expressing MT1 or MT2 receptors (CHO-hMelR7) were selected and cultured in Eagle’s Minimum Essential Medium-α (MEM-α) supplemented with 10% dialyzed fetal bovine serum (dFBS) under a 5% CO2/95% air atmosphere. Cells were harvested at confluence in Ca2+-Mg2+ free Hanks’ balanced salt solution containing 5 mM EDTA and collected by centrifugation. Cells were homogenized in ice-cold 50 mM Tris-HCl buffer (pH 7.7 at 25℃), washed twice, pelleted, and stored at -30℃ until the binding assays were conducted. Ramelteon and 40 pM 2-[125I]melatonin were mixed with the thawed homogenate in a total volume of 1 mL and incubated at 25℃ for 150 min. The reaction was terminated by addition of 3 mL of icecold buffer followed by vacuum filtration on a Whatman GF/B. The filter was washed twice and radioactivity was counted by a γ-counter. Nonspecific binding was defined as the binding in the presence of 10 mM melatonin. |
| Cell experiment [2]: | |
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Cell lines |
Pancreatic INS-1 β-cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reaction Conditions |
2-14 h |
|
Applications |
Ramelteon is a potent and selective agonist of MT1/MT2 melatonin receptors. Ramelteon inhibits forskolin-stimulated cAMP production in the CHO cells that express the human MT1 or MT2 receptors [2]. Ramelteon is capable of increasing brain-derived neurotrophic factor (BDNF) protein in neurons expressing either MT1 or MT2 receptor type in mouse cerebellar granule cells [3]. |
| Animal experiment [4]: | |
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Animal models |
Freely moving cats |
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Dosage form |
0.001, 0.01, and 0.1 mg/kg; administered orally. |
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Preparation method |
Suspended in a 0.5% (weight per volume) methylcellulose solution. |
|
Applications |
In cats, ramelteon has a sleep-promoting action and does not appear to cause learning, memory, or motor function impairment, or to have rewarding properties [4]. In a clinical study, ramelteon decreases latency to persistent sleep and increases total sleep time and sleep efficiency in subjects with primary chronic insomnia [1]. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Kato K, Hirai K, Nishiyama K, et al. Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology, 2005, 48(2): 301-310. [2]. Nishiyama K, Hirai K. The melatonin agonist ramelteon induces duration-dependent clock gene expression through cAMP signaling in pancreatic INS-1 β-cells. PLoS One, 2014, 9(7): e102073. [3]. Imbesi M, Uz T, Dzitoyeva S, et al. Stimulatory effects of a melatonin receptor agonist, ramelteon, on BDNF in mouse cerebellar granule cells. Neurosci Lett, 2008, 439(1): 34-36. [4]. Miyamoto M, Nishikawa H, Doken Y, et al. The sleep-promoting action of ramelteon (TAK-375) in freely moving cats. Sleep, 2004, 27(7): 1319-1325. | |
| Cas No. | 196597-26-9 | SDF | |
| Synonymes | TAK-375 | ||
| Chemical Name | N-[2-[(8S)-2,6,7,8-tetrahydro-1H-cyclopenta[e][1]benzofuran-8-yl]ethyl]propanamide | ||
| Canonical SMILES | CCC(=O)NCCC1CCC2=C1C3=C(C=C2)OCC3 | ||
| Formula | C16H21NO2 | M.Wt | 259.34 |
| Solubility | ≥ 12.95mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8559 mL | 19.2797 mL | 38.5594 mL |
| 5 mM | 0.7712 mL | 3.8559 mL | 7.7119 mL |
| 10 mM | 0.3856 mL | 1.928 mL | 3.8559 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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