Ramelteon (Synonyms: 雷美替胺; TAK-375)
目录号: PL07090 纯度: ≥99%
CAS No. :196597-26-9
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中文名称
Ramelteon
中文别名
雷美替胺;瑞美替昂;4-氯-2,6-二氟苯甲酸;拉米替隆-D5;雷美尔通;雷美替胺杂质;(S)-N-[2-(1,6,7,8-四氢-2H-茚并[5,4-b]呋喃-8-基)乙基]丙酰胺;(S)-N-[2-(2,6,7,8-四氢-1H-茚并[5,4-b]呋喃-8-基)乙基]丙酰胺;瑞美替胺;拉米替隆;瑞美替昂 -D5;雷美替胺 别名: RAMELTEON;瑞美替胺196597-26-9
英文名称
Ramelteon
英文别名
ramelteon;N-[2-[(8S)-2,6,7,8-tetrahydro-1H-cyclopenta[e][1]benzofuran-8-yl]ethyl]propanamide;Ramelteon solution;TAK-375;(S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide;[14C]-Ramelteon;Ramelteon [USAN];Rozerem;Rozerem (TN);Rozerem(TM);TAK375;UNII-901AS54I69;(S)-N-[2-(1,6,7,8-Tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide;N-[2-[(8S)-1,6,7,8-Tetrahydro-2H-indeno[5,4-b]furan-8-yl]ethyl]propanamide;(S)-N-[2-(2,6,7,8-Tetrahydro-1H-indeno[5,4-b]furan-8-yl)ethyl]propionamide;rac Rozerem;rac Ramelteon;RaMelteon(TAK-375);RAMELTEON(FORR&DONLY);TAK 375;Ramelteon, >=99%;Ramelteon (approx. 90% S);N-(2-(2,6,7,8-tetrahydro-1H-indeno[5,4-b]furan-8-yl)ethyl)propionamide;Remelteon;YLXDSYKOBKBWJQ-UHFFFAOYSA-N;DSSTox_RID_81247;DSSTox_CID_25951;DSSTox_GSID_45951;HMS3745O03;HMS3657C11;BCP18306;BCP04205;Tox21_111476;DISCONTINUED. See R110051';AK117788;A813859;L001280;Propanamide,N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan;Ramelteon
Cas No.
196597-26-9
分子式
C16H21NO2
分子量
259.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Ramelteon 是一种强效、高选择性和具有口服活性的 MT1/MT2 激动剂,Ki 值分别为 14 和 112 pM。Ramelteon 具有研究失眠症的潜力。Ramelteon长期使用持续减少睡眠发作,停药后无翌日晨残留效应或反弹性失眠或戒断症状。
生物活性
Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
性状
Solid
IC50 & Target[1][2]
MT2 MT1
体内研究(In Vivo)
Ramelteon (p.o.; 0.1 and 1 mg/kg) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle.
Ramelteon (p.o.; 3, 10, and 30 mg/kg) does not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential.
Ramelteon (0.0001, 0.001, 0.01, and 0.1 mg/kg; p.o.; 8 hours) 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Kato K, et al. Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 2005;48(2):301-310.
[2]. Mayer G, et al. Efficacy and safety of 6-month nightly ramelteon administration in adults with chronic primary insomnia. Sleep. 2009;32(3):351-360.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (192.80 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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