2. GPCR/G Protein Neuronal Signaling
  3. Melatonin Receptor
  4. Ramelteon

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.

Ramelteon Chemical Structure

Ramelteon Chemical Structure

CAS No. : 196597-26-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Ramelteon:

Ramelteon Related Antibodies

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MT1 MT2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

MT2

 

MT1

 

In Vivo

Ramelteon (p.o.; 0.1 and 1 mg/kg) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle[3].
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.

Animal Model: Male Wistar or Fischer 344 (F344) rats[3]
Dosage: 0.1 and 1 mg/kg; 3, 10, and 30 mg/kg
Administration: p.o.
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.
Animal Model: Adult cats (2.5-6.1 kg)[4]
Dosage: 0.0001, 0.001, 0.01, and 0.1 mg/kg
Administration: p.o.; 8 hours
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.
Clinical Trial
Molecular Weight

259.34

Formula

C16H21NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC[C@H]1C2=C(C=CC3=C2CCO3)CC1)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (192.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.87%

COA (253 KB) RP-HPLC (218 KB)

Handling Instructions (2659 KB)
References

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 3.8559 mL 19.2797 mL 38.5594 mL 96.3986 mL
5 mM 0.7712 mL 3.8559 mL 7.7119 mL 19.2797 mL
10 mM 0.3856 mL 1.9280 mL 3.8559 mL 9.6399 mL
15 mM 0.2571 mL 1.2853 mL 2.5706 mL 6.4266 mL
20 mM 0.1928 mL 0.9640 mL 1.9280 mL 4.8199 mL
25 mM 0.1542 mL 0.7712 mL 1.5424 mL 3.8559 mL
30 mM 0.1285 mL 0.6427 mL 1.2853 mL 3.2133 mL
40 mM 0.0964 mL 0.4820 mL 0.9640 mL 2.4100 mL
50 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.9280 mL
60 mM 0.0643 mL 0.3213 mL 0.6427 mL 1.6066 mL
80 mM 0.0482 mL 0.2410 mL 0.4820 mL 1.2050 mL
100 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.9640 mL
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Ramelteon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ramelteon196597-26-9TAK-375TAK375TAK 375Melatonin ReceptorMT1MT2oralinsomnianext-morning residual effectrebound insomniawithdrawal symptomdiscontinuationInhibitorinhibitorinhibit

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