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Fig. 1 · Structure
Cat. No.
A10777
CAS No.
196597-26-9
Formula
C16H21NO2
Mol. Weight
259.3

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Ramelteon (TAK-375)

Cat. No. A10777 CAS 196597-26-9

MT1/MT2-Receptor Agonist

Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ± 8.55 pM)and MT2 (20.1 ± 9.25 pM)receptors and selectivity over the MT3 receptor.

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Biological Activity

Target & Activity

Target Activity Value
MT1 receptor Ki 14 pM
MT receptor (chicken) Ki 23.1 pM
MT2 receptor Ki 112 pM

In Vitro Studies

In INS-1 cells, Ramelteon at 0.1–100 nM for 2 or 14 h significantly inhibited insulin secretion compared with vehicle-pretreated controls. In another study using INS-1 cells, Ramelteon significantly activated Rev-erbα mRNA expression in a time- and concentration-dependent manner. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Ramelteon inhibits insulin secretion in cultured cells

Cell-based study · INS-1 cells [1]

INS-1 cells received Ramelteon at 0.1–100 nM for 2 or 14 h. Both treatments significantly inhibited insulin secretion compared with vehicle-pretreated controls.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
insulin secretionReported result INS-1 cells were treated with ramelteon (0.1–100 nM) for 2 or 14 h. Both 2 and 14 h treatments with ramelteon significantly inhibited insulin secretion.[1]

Literature-Reported Treatment Conditions

Treatment concentration
0.1–100 nM
Exposure duration
for 2 or 14 h
Reported limits
Not stated in the sentences used: route, vehicle.
Methods and source locations

Compound reported in the paper: Ramelteon

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Comparisons of insulin secretion between short- and long-term treatments with ramelteon (S56); Figure 3 legend (S102, S106)

insulin secretion: insulin secretion; comparator: vehicle-pretreated controls — Results > Comparisons of insulin secretion between short- and long-term treatments with ramelteon (S56); Figure 3 legend (S102)

Activation of Rev-erbα expression

Cell-based study · INS-1 cells [1]

In INS-1 cells treated with Ramelteon at 1 nM, 10 nM, or 100 nM for 2 or 14 h, Rev-erbα mRNA expression was significantly activated in a time- and concentration-dependent manner.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
mRNA expression of Rev-erbαReported result Ramelteon significantly activated Rev-erbα expression in a time- and concentration-dependent manner[1]

Literature-Reported Treatment Conditions

Treatment concentration
1 nM, 10 nM, or 100 nM
Exposure duration
for 2 or 14 h
Reported limits
Not stated in the sentences used: route, vehicle.
Methods and source locations

Compound reported in the paper: Ramelteon

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Differences in clock gene expression between short- and long-term treatments with ramelteon (S62); Figure 5 legend (S111, S112)

mRNA expression of Rev-erbα: mRNA expression of Rev-erbα; comparator: vehicle-treated control — Results > Differences in clock gene expression between short- and long-term treatments with ramelteon (S62); Figure 5 legend (S111)

In Vivo Studies

In male mice undergoing middle cerebral artery occlusion, Ramelteon administered at 4 h after MCAO significantly reduced brain infarct volumes compared with vehicle. In male Sprague Dawley rats, Ramelteon was administered before VILI, and PaO2 concentration at 5 h after VILI was significantly higher in the VILI + ramelteon group than in the VILI group. [2,3]

Ramelteon reduces brain infarct volumes after cerebral ischemia

Animal study · Male C57BL/6 mice; middle cerebral artery occlusion (MCAO); n = 6 to 9 for each group [2]

Male mice undergoing middle cerebral artery occlusion received Ramelteon at 3.0 mg/kg i.g. at 4 h after MCAO. Ramelteon significantly reduced brain infarct volumes compared with vehicle.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Brain infarct volumesbrain infarct volumes Ram 4 h 36.2% ± 3.2% vs Vehicle 54.3% ± 1.9%[2]

Conditions shared by the study groups

Route
i.g.
Treatment course
Ramelteon was administered at 3.0 mg/kg at 4 h after MCAO. Brain infarct volumes and neurological deficit scores were determined 24 h after ischemia.
Vehicle
saline containing 0.5% carboxymethylcellulose (CMC)
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Ramelteon 3.0 mg/kgVehicleRamelteon significantly reduced brain infarct volumes as late as 4 h after ischemia (Ram 4 h 36.2% ± 3.2% vs Vehicle 54.3% ± 1.9%, P < 0.05[2]
Ramelteon 3.0 mg/kg
Model: Male C57BL/6 mice; middle cerebral artery occlusion (MCAO); n = 6 to 9 for each group
Methods and source locations

Compound reported in the paper: Ramelteon

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and methods > Animals (S1); Materials and methods > MCAO mouse model and the determination of ischemic injury (S4, S13); Materials and methods > Drug administration (S23, S25); Results > Effective time window of ramelteon in reducing MCAO-induced brain injury (S71); Fig. 2 legend (S124, S126, S127)

Brain infarct volumes: Brain infarct volumes; comparator: Vehicle — Results > Effective time window of ramelteon in reducing MCAO-induced brain injury (S71); Fig. 2 legend (S126)

Ramelteon 3.0 mg/kg · Materials and methods > Drug administration (S25); Results > Effective time window of ramelteon in reducing MCAO-induced brain injury (S71); Fig. 2 legend (S124, S126)

Ramelteon increases PaO2 in rats with ventilator-induced lung injury

Animal study · male Sprague Dawley rats; VILI; n = 6 per group [3]

Male Sprague Dawley rats received Ramelteon at 5 mg/kg by femoral vein injection 30 min before VILI. PaO2 concentration at 5 h after VILI was significantly higher in the VILI + ramelteon group than in the VILI group.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
PaO2 concentration at 5 h after VILIReported result The PaO2 concentration at 5 h after VILI was significantly higher in the VILI + ramelteon group than the VILI group.[3]

Conditions shared by the study groups

Route
femoral vein injection
Treatment course
30 min before VILI; ventilated with volume control for 5 h
Vehicle
0.3% ethanol in saline
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Ramelteon 5 mg/kgVILIThe PaO2 concentration at 5 h after VILI was significantly higher in the VILI + ramelteon group than the VILI group.[3]
Ramelteon 5 mg/kg
Model: male Sprague Dawley rats; VILI; n = 6 per group
Reported limits: Removed after verification: value.
Methods and source locations

Compound reported in the paper: Ramelteon

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Methods > Animals (S1); Methods > Experimental protocols (S4, S8, S10, S13, S14, S15); Results > Effect of melatonin and ramelteon on oxygenation (S52); Table 1 legend (S169); Table 1 (T1.h1, T1.r5, T1.r9)

PaO2 concentration at 5 h after VILI: PaO2 concentration at 5 h after VILI; comparator: VILI — Results > Effect of melatonin and ramelteon on oxygenation (S52); Table 1 legend (S169); Table 1 (T1.h1, T1.r9)

Ramelteon 5 mg/kg · Methods > Experimental protocols (S8, S10, S13); Results > Effect of melatonin and ramelteon on oxygenation (S52); Table 1 legend (S169); Table 1 (T1.r9)

Specifications

Manufacturer Adooq Bioscience
Actions Agonist
CAS Number 196597-26-9
Applications MT1/MT2-Receptor Agonist
Formula C16H21NO2
Molecular Weight 259.3
Synonyms Rozerem; TAK-375
SMILES
CCC(=O)NCC[C@@H]1CCC2=C1C3=C(C=C2)OCC3

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 47 mg/mL (181.22 mM)
Water Insoluble
Ethanol 47 mg/mL (181.22 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
0.5% methylcellulose

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] 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). PMID: 25013953 DOI: 10.1371/journal.pone.0102073 Source material
  2. [2] Wu XL, Lu SS, Liu MR, et al. Melatonin receptor agonist ramelteon attenuates mouse acute and chronic ischemic brain injury. Acta Pharmacol Sin (2020). PMID: 32107468 DOI: 10.1038/s41401-020-0361-2 Source material
  3. [3] Wu GC, Peng CK, Liao WI, et al. Melatonin receptor agonist protects against acute lung injury induced by ventilator through up-regulation of IL-10 production. Respir Res (2020). PMID: 32143642 DOI: 10.1186/s12931-020-1325-2 Source material

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