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Synonyms | TAK-375 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H21NO2 |
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分子量 | 259.34 | CAS No. | 196597-26-9 | ||||
Solubility (25°C)* | 体外 | DMSO | 51 mg/mL (196.65 mM) | ||||
Ethanol | 51 mg/mL (196.65 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Ramelteon (TAK-375) 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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in vitro | Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. [1] 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. [2] 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. [3] |
in vivo | 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. [2] 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. [4] 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. [5] |
特徴 | A tricyclic synthetic analog of melatonin. |
キナーゼアッセイ | Binding assays | |
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Cells expressing the tested receptor are selected and cultured in Eagle's Minimum Essential Medium-α (MEM-α) supplemented with 10% dialyzed fetal bovine serum (dFBS) under a 5% CO2/95% air atmosphere. Cells are harvested at confluence in Ca2+-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 (pH 7.7 at 25 ℃), washed twice, pelleted, and stored at −30 ℃ until the binding assays are conducted. Ramelteon and 40 pM 2-[125I]melatonin are mixed with the thawed homogenate in a total volume of 1 mL and incubated at 25 ℃ for 150 min. The reaction is terminated by addition of 3 mL of ice-cold buffer followed by vacuum filtration on a Whatman GF/B. The filter is washed twice and radioactivity is counted by a γ-counter. Nonspecific binding is defined as the binding in the presence of 10 μM melatonin. | ||
動物実験 | 動物モデル | estrogen-deficient ovariectomized (OVX) rats |
投薬量 | 1 mg/kg | |
投与方法 | Orally |
Data from [Data independently produced by , , Free Radic Biol Med, 2018, 131:345-355]
Data from [Data independently produced by , , PLoS One, 2016, 11(11):e0166442.]
Data from [Data independently produced by , , PLoS One, 2016, 11(11):e0166442]
Microglial MT1 activation inhibits LPS-induced neuroinflammation via regulation of metabolic reprogramming [ Aging Cell, 2021, e13375] | PubMed: 33964119 |
Energy restriction causes metaphase delay and chromosome mis-segregation in cancer cells [ Cell Cycle, 2021, 20(12):1195-1208] | PubMed: 34048314 |
SlSNAT interacts with HSP40, a molecular chaperone, to regulate melatonin biosynthesis and promote thermotolerance in tomato. [ Plant Cell Physiol, 2020, 10.1093/pcp/pcaa018] | PubMed: 32065633 |
Controlling distinct signaling states in cultured cancer cells provides a new platform for drug discovery [ FASEB J, 2019, 10.1096/fj.201802603RR] | PubMed: 31145643 |
Melatonin receptor activation provides cerebral protection after traumatic brain injury by mitigating oxidative stress and inflammation via the Nrf2 signaling pathway [Wang J Free Radic Biol Med, 2018, 131:345-355] | PubMed: 30553970 |
Melatonin Receptor Agonists as the “Perioceutics” Agents for Periodontal Disease through Modulation of Porphyromonas gingivalis Virulence and Inflammatory Response [Zhou W PLoS One, 2016, 11(11):e0166442] | PubMed: 27832188 |
Establishment and assessment of a new human embryonic stem cell-based biomarker assay for developmental toxicity screening. [Palmer JA Birth Defects Res B Dev Reprod Toxicol, 2013, 98(4):343-63] | PubMed: 24123775 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。