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

Ramelteon (Synonyms: TAK-375)

Cat. No.: HY-A0014 Purity: 99.92% ee.: 100.00%
Handling Instructions

Ramelteon is a highly potent and selective melatonin receptor agonist with Ki values of 14 and 112 pM for human melatonin1 and melatonin2.

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 USD 82 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 100 In-stock
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50 mg USD 260 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ramelteon is a highly potent and selective melatonin receptor agonist with Ki values of 14 and 112 pM for human melatonin1 and melatonin2.

IC50 & Target

IC50: 14 pM (melatonin1), 112 pM (melatonin2)[1]

In Vitro

Ramelteon shows very high affinity for human melatonin1 and melatonin2 receptors (expressed in CHO cells), and chick forebrain melatonin receptors (consisting of melatonin1 and melatonin2 receptors) with Ki values of 14.0, 112, and 23.1 pM, respectively. The affinity of ramelteon for hamster brain melatonin3 binding sites is extremely weak (Ki: 2.65 μM) compared to melatonin's affinity for the melatonin3 binding site Ki: 24.1 nM). In addition, ramelteon shows no measurable affinity for a large number of ligand binding sites (including benzodiazepine receptors, dopamine receptors, opiate receptors, ion channels, and transporters) and no effect on the activity of various enzymes. Ramelteon inhibits forskolin-stimulated cAMP production in the CHO cells that express the human melatonin1 and melatonin2 receptors[1].

In Vivo

Ramelteon 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 in freely moving cats[2]. Ramelteon is associated with reduced subjective sleep latency and improved sleep quality. Ramelteon is associated with improvement in latency to persistent sleep, sleep efficiency , and total sleep time[3]. Ramelteon (10 mg/kg, i/p), administered close to the mid-point of the dark phase of the L:D cycle, significantly reduces NREM sleep latency (time from injection to the appearance of NREM sleep). Ramelteon also produces a short-lasting increase in NREM sleep duration, but the NREM power spectrum is unaltered[4].

Clinical Trial
Molecular Weight

259.34

Formula

C₁₆H₂₁NO₂

CAS No.

196597-26-9

SMILES

O=C(NCC[[email protected]]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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (192.80 mM)

*"≥" 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
10 mM 0.3856 mL 1.9280 mL 3.8559 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

cDNA encoding the human MT1 gene is introduced into CHO cells. Cells are harvested at confluence in Ca2+ and Mg2+ free Hanks’ balanced salt solution containing 5 mM EDTA and collected by centrifugation. Cells are homogenized in ice-cold 50 mM Tris–HCl buffer, washed twice, pelleted, and stored at -30°C until the binding assays are conducted. Test compound and 40 pM 2-[ 125I]melatonin are mixed with the thawed homogenate in a total volume of 1 mL and incubated at 25°C for 150 min. The reaction is terminated by addition of 3 mL of icecold buffer followed by vacuum filtration on a Whatman GF/B. The filter is washed twice and radioactivity is counted by a g-counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Rats: Ramelteon is dissolved in DMSO at a concentration of 200 mg/mL, and diluted 100-fold in physiological saline immediately before use. A different group of six implanted rats is given vehicle or ramelteon (10 mg/kg i.p.). The EEG and EMG are recorded for 1 hr before injection and then for a further 3.5 hr. All treatments are administered at 24:00 hr (near the mid-point of the dark phase of the L:D cycle) with a minimum of 72 hr separating injections in the same animal. Each rat receives both treatments in a fully randomized, balanced cross-over design reducing the number of animals needed in the study[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.92% ee.: 100.00%

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Keywords:

RamelteonTAK-375TAK375TAK 375Melatonin ReceptorInhibitorinhibitorinhibit

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