化合物 Ramelteon metabolite M-II|T12689|TargetMol

Ramelteon metabolite M-II
896736-21-3

￥1620 1mg 起订

￥8780 10mg 起订

￥4810 5mg 起订

上海更新日期：2024-09-29

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产品详情:

中文名称：: 化合物 Ramelteon metabolite M-II

英文名称：: Ramelteon metabolite M-II

CAS号：: 896736-21-3

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

产品类别：: 抑制剂

货号：: T12689

Product Introduction

Bioactivity

名称	Ramelteon metabolite M-II
描述	Ramelteon metabolite M-II is the primary metabolite of Ramelteon and exhibits IC50 values of 208 pM and 1470 pM for human melatonin receptors (MT1 and MT2), respectively. Ramelteon itself is a selective melatonin receptor agonist.
体外活性	The affinity of Ramelteon metabolite M-II (M-II) for MT1 receptors is 10- and 2.5-fold lower than that of ramelteon and melatonin, respectively, and for MT2 receptors is approximately 5- and 1.5-fold lower. The selectivity of M-II for melatonin receptors over 215 targets, including other receptors, transporters, ion channels, and enzymes, was investigated. No significant affinities or activities were observed for these targets, except for the 5-HT2B receptor, with a Ki value of 1.75±0.23 μM. The potency of M-II for MT1 receptors is approximately 17- and 4.3-fold lower than that of ramelteon and melatonin, respectively, and for MT2 receptors is approximately 28- and 1.6-fold lower.
体内活性	Ramelteon metabolite M-II 1 mg/kg significantly increases NREM sleep and significantly decreases wakefulness. Moreover, a lower dose of M-II (0.1 mg/kg) yield similar results (NREM, F1,7=121.9, p<0.01; wakefulness, F1,7=87.0, p<0.01), and decreased wakefulness is sustained for 6 h after the administration of either dose. After the administration of 0.01 mg/kg M-II, only NREM sleep is significantly increased . No significant differences in REM sleep are observed after the administration of M-II at any of the doses tested in this study.
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
关键字	Ramelteon metabolite MII \| Ramelteon metabolite M II \| Ramelteon metabolite M-II

Ramelteon metabolite M-II|TargetMol

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