Ramelteon

製品コードS1259 バッチS125902

印刷

化学情報

Chemical Structure Synonyms TAK-375 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H21NO2
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
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assays
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

カスタマーフィードバック

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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