产品说明书

Ramelteon

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Chemical Structure| 196597-26-9 同义名 : TAK-375
CAS号 : 196597-26-9
货号 : A428570
分子式 : C16H21NO2
纯度 : 98%
分子量 : 259.343
MDL号 : MFCD08067736
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(192.79 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
描述 Ramelteon, a potent and highly selective MT1/MT2 receptor agonist with Ki values of 14 and 112 pM respectively, is orally active and has potential for insomnia research. It consistently lowers the time it takes to fall asleep over prolonged use without causing any residual effects the next morning, or symptoms of rebound insomnia or withdrawal after stopping[1].[2].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00642694 - Terminated(Enrollment disconti... 展开 >>nued based on mutually agreed upon decision by PI and funding sponsor) 收起 << - -
NCT02969343 Central Line-Associated Bloods... 展开 >>tream Infection (CLABSI) Venous Thromboembolism Patient Fall Catheter-Associated Infection Severe Hypoglycemia Opioid-Related Severe Adverse Drug Event Hospital Acquired Pressure Ulcer Adverse Drug Event Severe Hospital Acquired Delerium Rapid Response Related to Arrhythmia 收起 << Not Applicable Recruiting September 2018 United States, Massachusetts ... 展开 >> Brigham and Women's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Alexandra C Businger    617-732-7063    abusinger@partners.org    Contact: Patricia Dykes, RN PhD    617-732-8925    pdykes@partners.org    Principal Investigator: David W Bates, MD MSc 收起 <<
NCT00893269 Marijuana Dependence Phase 1 Completed - United States, Maryland ... 展开 >> Johns Hopkins University Baltimore, Maryland, United States, 21224 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.86mL

0.77mL

0.39mL

19.28mL

3.86mL

1.93mL

38.56mL

7.71mL

3.86mL

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.

[3]Hirai K, et al. Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats. J Biol Rhythms. 2005;20(1):27-37.

[4]Miyamoto M, et al. The sleep-promoting action of ramelteon (TAK-375) in freely moving cats. Sleep. 2004;27(7):1319-1325.