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其他生物化学试剂

化合物 T12689 T12689

英文名称:Ramelteon metabolite M-II
品牌 厂商性质 产地 货期
TargetMol 生产商 美国 现货

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生化试剂,可用于动物细胞实验

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规格 CAS号 价格 操作
1 mg 896736-21-3 ¥1,620.00 询底价
10 mg 896736-21-3 ¥8,780.00 询底价
5 mg 896736-21-3 ¥4,810.00 询底价
产品介绍

Product Introduction
Bioactivity


英文名: Ramelteon metabolite M-II

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.

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

关键字: Ramelteon metabolite MII | Ramelteon metabolite M II | Ramelteon metabolite M-II

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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途

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