Ramelteon (Synonyms:雷美替胺; TAK-375)
目录号 : KM18106 CAS No. : 196597-26-9 纯度 : 98%

Ramelteon是高效选择性的melatonin受体激动剂,结合人melatonin1和melatonin2受体的Ki值分别为14 和112 pM。

规格 价格 是否有货 数量
2mg
In-stock
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Ramelteon is a highly potent and selective melatonin receptor agonist with Ki values of 14 and 112 pM for human melatonin1 and 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: 2.65 μM) compared to melatonin's affinity for the melatonin3 binding site Ki: 24.1 nM). 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 0.1 mg/kg, increases slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increases rapid eye movement sleep at a dose of 0.1 mg/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 (10 mg/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.

分子式
C16H21NO2
分子量
259.34
CAS号
196597-26-9
中文名称
雷美替胺;瑞美替昂;拉米替隆;雷美尔通;瑞美替胺
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (192.80 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8559 mL 19.2797 mL 38.5594 mL
5 mM 0.7712 mL 3.8559 mL 7.7119 mL
10 mM 0.3856 mL 1.9280 mL 3.8559 mL
*

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。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.64 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.64 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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