Ramelteon
Based on 12 publication(s) in Google Scholar
Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 196597-26-9
- Formula: C16H21NO2
- Molecular Weight:259.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ramelteon
More- Nat Commun. 2025 Nov 6;16(1):9812. [Abstract]
- Nat Commun. 2022 Jan 24;13(1):454. [Abstract]
- Acta Pharmacol Sin. 2020 Aug;41(8):1016-1024. [Abstract]
- Ecotoxicol Environ Saf. 2021 Jan 1:207:111561. [Abstract]
- Chem Biol Interact. 2022 Sep 25:365:110085. [Abstract]
- Inflammation. 2025 Jan 3. [Abstract]
- Eur J Pharmacol. 2025 Jul 5:998:177498. [Abstract]
- Int Immunopharmacol. 2022 Aug:109:108778. [Abstract]
- Drug Metab Dispos. 2025 Dec 22.
- Neurotox Res. 2021 Jun;39(3):677-686. [Abstract]
- Cell Biochem Biophys. 2025 Jun;83(2):2289-2299. [Abstract]
- Biol Pharm Bull. 2019;42(2):280-288. [Abstract]
Biological Activity
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MT2 |
MT1 |
Ramelteon (p.o.; 3, 10, and 30 mg/kg) does not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential[3].
Ramelteon (0.0001, 0.001, 0.01, and 0.1 mg/kg; p.o.; 8 hours) significantly decreases wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, increases slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increases rapid eye movement sleep at a dose of 0.1 mg/kg[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar or Fischer 344 (F344) rats[3]
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Dosage:0.1 and 1 mg/kg; 3, 10, and 30 mg/kg
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Administration:p.o.
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Result:Accelerated reentrainment of running wheel activity rhythm to the new lightdark cycle. Ramelteon did not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential.
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Animal Model:Adult cats (2.5-6.1 kg)[4]
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Dosage:0.0001, 0.001, 0.01, and 0.1 mg/kg
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Administration:p.o.; 8 hours
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Result:Significantly decreased wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, increased slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increased rapid eye movement sleep at a dose of 0.1 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 196597-26-9
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Appearance Solid
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Molecular Weight 259.35
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Formula C16H21NO2
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Color White to off-white
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SMILES
O=C(NCC[C@H]1C2=C(C=CC3=C2CCO3)CC1)CC
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Synonyms
TAK-375
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 Nov 6;16(1):9812. PMID: 41198646 -
Nat Commun
2022 Jan 24;13(1):454. PMID: 35075127 -
Acta Pharmacol Sin
Melatonin receptor agonist ramelteon attenuates mouse acute and chronic ischemic brain injury. [Abstract]2020 Aug;41(8):1016-1024. PMID: 32107468 -
Ecotoxicol Environ Saf
Melatonin alleviates benzo(a)pyrene-induced ovarian corpus luteum dysfunction by suppressing excessive oxidative stress and apoptosis. [Abstract]2021 Jan 1:207:111561. PMID: 33254415 -
Chem Biol Interact
Exposure to Benzo(a)pyrene damages mitochondrial function via suppressing mitochondrial melatonin receptors in ovarian corpus luteum during early pregnancy. [Abstract]2022 Sep 25:365:110085. PMID: 35940284 -
Inflammation
2025 Jan 3. PMID: 39751706 -
Eur J Pharmacol
Parishin A alleviates insomnia by regulating hypothalamic-pituitary-adrenal axis homeostasis and directly targeting orexin receptor OX2. [Abstract]2025 Jul 5:998:177498. PMID: 40064224 -
Int Immunopharmacol
Melatonin relieves Th17/CD4-CD8- T cells inflammatory responses via nuclear-receptor dependent manner in peripheral blood of primary Sjögren's syndrome. [Abstract]2022 Aug:109:108778. PMID: 35537347 -
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Neurotox Res
The Protective Effects of Ramelteon Against Isoflurane-Induced Insults and Inflammatory Response in Brain Microvascular Endothelial Cells. [Abstract]2021 Jun;39(3):677-686. PMID: 33211285 -
Cell Biochem Biophys
Indoleamine 2, 3-dioxygenase Regulates the Differentiation of T Lymphocytes to Promote the Growth of Gastric Cancer Cells through the PI3K/Akt/mTOR Pathway. [Abstract]2025 Jun;83(2):2289-2299. PMID: 39695014 -
Biol Pharm Bull
Assessment of Inhibitory Effects of Hypnotics on Acetylcholine-Induced Contractions in Isolated Rat Urinary Bladder Smooth Muscle. [Abstract]2019;42(2):280-288. PMID: 30713259
Solvent & Solubility
DMSO : 100 mg/mL (385.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Kato K, et al. Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 2005;48(2):301-310. [Content Brief]
[2]. Mayer G, et al. Efficacy and safety of 6-month nightly ramelteon administration in adults with chronic primary insomnia. Sleep. 2009;32(3):351-360. [Content Brief]
[3]. Hirai K, et al. Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats. J Biol Rhythms. 2005;20(1):27-37. [Content Brief]
[4]. Miyamoto M, et al. The sleep-promoting action of ramelteon (TAK-375) in freely moving cats. Sleep. 2004;27(7):1319-1325. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8558 mL | 19.2790 mL | 38.5581 mL | 96.3952 mL |
| 5 mM | 0.7712 mL | 3.8558 mL | 7.7116 mL | 19.2790 mL | |
| 10 mM | 0.3856 mL | 1.9279 mL | 3.8558 mL | 9.6395 mL | |
| 15 mM | 0.2571 mL | 1.2853 mL | 2.5705 mL | 6.4263 mL | |
| 20 mM | 0.1928 mL | 0.9640 mL | 1.9279 mL | 4.8198 mL | |
| 25 mM | 0.1542 mL | 0.7712 mL | 1.5423 mL | 3.8558 mL | |
| 30 mM | 0.1285 mL | 0.6426 mL | 1.2853 mL | 3.2132 mL | |
| 40 mM | 0.0964 mL | 0.4820 mL | 0.9640 mL | 2.4099 mL | |
| 50 mM | 0.0771 mL | 0.3856 mL | 0.7712 mL | 1.9279 mL | |
| 60 mM | 0.0643 mL | 0.3213 mL | 0.6426 mL | 1.6066 mL | |
| 80 mM | 0.0482 mL | 0.2410 mL | 0.4820 mL | 1.2049 mL | |
| 100 mM | 0.0386 mL | 0.1928 mL | 0.3856 mL | 0.9640 mL |
Ramelteon Related Classifications
HY-A0014 Related Classifications
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