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Ramelteon metabolite M-II

产品编号 T12689 CAS 896736-21-3

Ramelteon metabolite M-II is the major Ramelteon metabolite(human melatonin receptors (MT1 or MT2) with IC50s of 208 pM, 1470 pM). Ramelteon is an agonist of selective melatonin.

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Ramelteon metabolite M-II Chemical Structure

Ramelteon metabolite M-II, CAS 896736-21-3

规格	价格/CNY	货期
1 mg	￥ 1,620	35日内发货
5 mg	￥ 4,810	35日内发货
10 mg	￥ 8,780	35日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Ramelteon metabolite M-II is the major Ramelteon metabolite(human melatonin receptors (MT1 or MT2) with IC50s of 208 pM, 1470 pM). Ramelteon is an agonist of selective melatonin.
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. Likewise, the affinity of M-II for MT2 receptors is approximately 5- and 1.5-fold lower than that of ramelteon and melatonin, respectively. The selectivity of M-II for melatonin receptors relative to 215 targets including other receptors, transporters, ion channels and enzymes is investigated. M-II shows no significant affinities and activities for the other targets, except for the 5-HT2B receptor, for which the Ki value was 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. Similarly, the potency of M-II for MT2 receptors is approximately 28- and 1.6-fold lower than that of ramelteon and melatonin, respectively.
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.

分子量	275.34
分子式	C16H21NO3
CAS No.	896736-21-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Nishiyama K, et al. Pharmacological characterization of M-II, the major human metabolite of ramelteon. Pharmacology. 2014;93(3-4):197-201.

剂量换算

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

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体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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