中文名称: | Ramelteon | ||||
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英文名称: | Ramelteon | ||||
别名: | 雷美替胺;(S)-N-(2-(2,6,7,8-四氢-1H-茚并[5,4-b]呋喃-8-基)乙基)丙酰胺 (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide | ||||
CAS No: | 196597-26-9 | 分子式: | C16H21NO2 | 分子量: | 259.34 |
CAS No: | 196597-26-9 | ||||
分子式: | C16H21NO2 | ||||
分子量: | 259.34 |
基本信息
产品编号: |
R20003 |
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产品名称: |
Ramelteon |
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CAS: |
196597-26-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
259.34 |
-20℃ |
1个月 |
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化学名: |
(S)-N-(2-(2,6,7,8-四氢-1H-茚并[5,4-b]呋喃-8-基)乙基)丙酰胺(S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide |
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Solubility (25°C): |
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体外:
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DMSO |
52mg/mL (200.5mM) |
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Ethanol |
52mg/mL (200.5mM) |
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Water |
Insoluble |
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体内(现配现用): |
0.5% methylcellulose |
30mg/mL |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.8559mL |
19.2797mL |
38.5594mL |
5mM |
0.7712mL |
3.8559mL |
7.7119mL |
10mM |
0.3856mL |
1.9280mL |
3.8559mL |
50mM |
0.0771mL |
0.3856mL |
0.7712mL |
生物活性
产品描述 |
一种高效选择性的melatonin受体激动剂,结合人melatonin1和melatonin2受体的Ki值分别为14 和112pM。 |
靶点 |
14pM (melatonin1),112pM (melatonin2) |
体外研究 |
Ramelteon shows very high affinity for human melatonin1 and melatonin2 receptors (expressed in CHO cells),and chick forebrain melatonin receptors (consisting of melatonin1 and melatonin2 receptors) with Ki values of 14.0,112,and 23.1 pM,respectively.The affinity of ramelteon for hamster brain melatonin3 binding sites is extremely weak (Ki:2.65μM) compared to melatonin's affinity for the melatonin3 binding site Ki:24.1nM).In addition,ramelteon shows no measurable affinity for a large number of ligand binding sites (including benzodiazepine receptors,dopamine receptors,opiate receptors,ion channels,and transporters) and no effect on the activity of various enzymes.Ramelteon inhibits forskolin-stimulated cAMP production in the CHO cells that express the human melatonin1 and melatonin2 receptors. |
体内研究 |
Ramelteon significantly decreases wakefulness at doses of 0.001,0.01,and 0.1mg/kg,increases slow-wave sleep at doses of 0.001,0.01,and 0.1mg/kg,and increases rapid eye movement sleep at a dose of 0.1mg/kg in freely moving cats.Ramelteon is associated with reduced subjective sleep latency and improved sleep quality.Ramelteon is associated with improvement in latency to persistent sleep,sleep efficiency ,and total sleep time.Ramelteon (10mg/kg,i/p),administered close to the mid-point of the dark phase of the L:D cycle,significantly reduces NREM sleep latency (time from injection to the appearance of NREM sleep).Ramelteon also produces a short-lasting increase in NREM sleep duration,but the NREM power spectrum is unaltered. |
推荐实验方法(仅供参考)
激酶实验: |
cDNA encoding the human MT1 gene is introduced into CHO cells.Cells are harvested at confluence in Ca2+and Mg2+free Hanks’balanced salt solution containing 5mM EDTA and collected by centrifugation.Cells are homogenized in ice-cold 50mM Tris–HCl buffer, washed twice, pelleted, and stored at -30℃ until the binding assays are conducted.Test compound and 40 pM 2-[ 125I]melatonin are mixed with the thawed homogenate in a total volume of 1mL and incubated at 25℃ for 150 min.The reaction is terminated by addition of 3mL of icecold buffer followed by vacuum filtration on a Whatman GF/B.The filter is washed twice and radioactivity is counted by a g-counter. |
动物实验: |
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Rats: Ramelteon is dissolved in DMSO at a concentration of 200mg/mL,and diluted 100-fold in physiological saline immediately before use.A different group of six implanted rats is given vehicle or ramelteon (10mg/kg i.p.).The EEG and EMG are recorded for 1hr before injection and then for a further 3.5hr.All treatments are administered at 24:00hr (near the mid-point of the dark phase of the L:D cycle) with a minimum of 72hr separating injections in the same animal.Each rat receives both treatments in a fully randomized,balanced cross-over design reducing the number of animals needed in the study. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )