Ramelteon

  Cat. No.:  DC7828  
Chemical Structure
196597-26-9
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More than 5000 active chemicals with high quality for research!
Field of application
Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.
Cas No.: 196597-26-9
Chemical Name: (S)-N-[2-(1,6,7,8-Tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide
Synonyms: TAK-375; Rozerem; TAK375; TAK 375,
SMILES: O=C(NCC[C@H]1C2=C(C=CC3=C2CCO3)CC1)CC
Formula: C16H21NO2
M.Wt: 259.34
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. Ramelteon has high affinity with recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. Ramelteon inhibits Xenopus laevis melanophore pigment granule aggregation with pEC50 of 11.48. Ramelteon (1 nM) increases ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells but also in cerebellar granule cells expressing only one of the two melatonin receptors. 4P-PDOT blocks the stimulatory action of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, while luzindole attenuates the action of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon (100 μM) induces any pigment dispersion while melatonin completely disperses aggregated melanophores at 10 μM. Ramelteon (10 mg/kg, i/p) significantly reduces NREM sleep latency in rat and also produces a short-lasting increase in nonrapid eye movement (NREM) sleep duration, but the NREM power spectrum is unaltered. Ramelteon (0.1 mg/kg and 1 mg/kg, p.o.) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle in rats without affecting learning or memory. Ramelteon (0.03 mg/kg and 0.3 mg/kg, p.o.) significantly shortens latency to sleep onset and significantly increases total duration of sleep in freely moving monkeys without affecting the general behavior of the monkeys. For the detailed information of Ramelteon, the solubility of Ramelteon in water, the solubility of Ramelteon in DMSO, the solubility of Ramelteon in PBS buffer, the animal experiment (test) of Ramelteon, the cell expriment (test) of Ramelteon, the in vivo, in vitro and clinical trial test of Ramelteon, the EC50, IC50,and affinity,of Ramelteon, Please contact DC Chemicals.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC46847 DH97 DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses.
DC46846 UCM 608 UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4.
DC46453 6-Chloromelatonin 6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. 6-Chloromelatonin compete for [3H]-melatonin and 2-[125I]-iodomelatonin binding to MT1 receptors (pKi=8.9 and 9.1, respectively). 6-Chloromelatonin compete for [3H]-melatonin binding to MT2 receptors (pKi=9.77).
DC28727 7-Desmethyl-3-hydroxyagomelatine 7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist.
DC28432 S26131 S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.
DC28122 8-M-PDOT 8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity.
DC28114 2-Iodomelatonin 2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1  over MT2. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.
DC7828 Ramelteon Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.
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