Ramelteon metabolite M-II

Name: Ramelteon metabolite M-II
Brand: MedChemExpress
SKU: HY-103005
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製品番号: HY-103005 純度: 98.84%: Data Sheet SDS COA 取扱説明書
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Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC₅₀s of 208 pM, 1470 pM for human melatonin receptors (MT₁ or MT₂). Ramelteon is a selective melatonin agonist.

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Ramelteon metabolite M-II 構造式

CAS 番号 : 896736-21-3

容量	価格（税別）	在庫状況	数量
5 mg	$287	在庫あり	Estimated Time of Arrival: December 31
10 mg	$460	在庫あり	Estimated Time of Arrival: December 31
25 mg	$912	在庫あり	Estimated Time of Arrival: December 31
50 mg		お問い合わせ
100 mg		お問い合わせ

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カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of Ramelteon metabolite M-II:

Ramelteon metabolite M-II-d₃ 在庫あり
Ramelteon metabolite M-II (Standard) お問い合わせ

Melatonin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

MT1 MT2

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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

体外実験

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. Ramelteon metabolite M-II exhibits no affinity for quinone reductase 2 at concentrations up to 10 μM. Moreover, the selectivity of Ramelteon metabolite M-II for melatonin receptors relative to 215 targets including other receptors, transporters, ion channels and enzymes is investigated. Ramelteon metabolite M-II shows no significant affinities and activities for the other targets, except for the 5-HT_2B receptor, for which the Ki value was 1.75±0.23 μM. The potency of Ramelteon metabolite M-II for MT₁ receptors is approximately 17- and 4.3-fold lower than that of ramelteon and melatonin, respectively. Similarly, the potency of Ramelteon metabolite M-II for MT₂ receptors is approximately 28- and 1.6-fold lower than that of ramelteon and melatonin, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Ramelteon metabolite M-II (1 mg/kg) significantly increases NREM sleep (F_1,7=96.3, p<0.01) and significantly decreases wakefulness (F_1,7=56.7, p<0.01). Moreover, a lower dose of M-II (0.1 mg/kg) yield similar results (NREM, F_1,7=121.9, p<0.01; wakefulness, F_1,7=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 Ramelteon metabolite M-II, only NREM sleep is significantly increased (F_1,7=10.5, p< 0.05). No significant differences in REM sleep are observed after the administration of M-II at any of the doses tested in this study^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

275.34

分子式

C₁₆H₂₁NO₃

CAS 番号

896736-21-3

Appearance

Solid

Color

White to off-white

SMILES

CC(O)C(NCC[C@@H]1CCC2=CC=C3OCCC3=C12)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (363.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6319 mL	18.1594 mL	36.3187 mL
5 mM	0.7264 mL	3.6319 mL	7.2637 mL
10 mM	0.3632 mL	1.8159 mL	3.6319 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (18.16 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (18.16 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (18.16 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 98.84%

Select Batch:

データシート (279 KB) SDS (393 KB)

COA (255 KB) HNMR (138 KB) LCMS (325 KB)

取扱説明書 (2659 KB)

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. [Content Brief]

動物実験
^[1]

Cats^[1]
Eight adult cats weighing 2.4-5.9 kg are used in each study. The cats are housed individually in rooms maintained at 22-26 °C with a 12-h light-dark cycle (lights on at 7.00 a.m.), fed once daily (9.00 a.m.) and given water ad libitum. The cats are anesthetized, and electrodes are surgically implanted for electroencephalogram (EEG), electromyogram (EMG) and electrooculogram (EOG) monitoring. After a recovery period of at least 7 days, the cats are well accustomed to the test chamber (65×35×45 cm). Ramelteon metabolite M-II is orally administered at 0.1 mL/kg to each cat using gelatin capsules. The effects of M-II on sleep are compared with those of the vehicle using a crossover design. The interval between trials is >6 days. The cats are given Ramelteon metabolite M-II (0.001, 0.01, 0.1 or 1 mg/kg) or vehicle between 9.55 and 10.00 a.m. Immediately after the administration, EEG, EOG and EMG recordings are started sequentially and lasted 8 h. The durations of sleep stages are measured after the administration of vehicle or M-II and are presented as mean percentages of time spent in each stage at each 2-hour period after administration^[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.6319 mL	18.1594 mL	36.3187 mL	90.7968 mL
	5 mM	0.7264 mL	3.6319 mL	7.2637 mL	18.1594 mL
	10 mM	0.3632 mL	1.8159 mL	3.6319 mL	9.0797 mL
	15 mM	0.2421 mL	1.2106 mL	2.4212 mL	6.0531 mL
	20 mM	0.1816 mL	0.9080 mL	1.8159 mL	4.5398 mL
	25 mM	0.1453 mL	0.7264 mL	1.4527 mL	3.6319 mL
	30 mM	0.1211 mL	0.6053 mL	1.2106 mL	3.0266 mL
	40 mM	0.0908 mL	0.4540 mL	0.9080 mL	2.2699 mL
	50 mM	0.0726 mL	0.3632 mL	0.7264 mL	1.8159 mL
	60 mM	0.0605 mL	0.3027 mL	0.6053 mL	1.5133 mL
	80 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1350 mL
	100 mM	0.0363 mL	0.1816 mL	0.3632 mL	0.9080 mL