Ramelteon metabolite M-II
(Synonyms: 雷美替胺杂质) 目录号 : GC37070
A mixed isomer preparation of ramelteon metabolite M-II
Cas No.:896736-21-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(R,S)-hydroxy Ramelteon metabolite M-II is a mixed isomer preparation of the melatonin receptor agonist ramelteon metabolite M-II, which is a metabolite of ramelteon .1,2 It has an (R,S) configuration at the hydroxy group, where ramelteon metabolite M-II has the (S) configuration at that position.
1.Nishiyama, K., Nishikawa, H., Kato, K., et al.Pharmacological characterization of M-II, the major human metabolite of ramelteonPharmacology93(3-4)197-201(2014) 2.Nishiyama, K., and Hirai, K.In vitro comparison of duration of action of melatonin agonists on melatonin MT1 receptor: Possible link between duration of action and dissociation rate from receptorEur. J. Pharmacol.75742-52(2015)
| Cas No. | 896736-21-3 | SDF | |
| 别名 | 雷美替胺杂质 | ||
| Canonical SMILES | CC(O)C(NCC[C@@H]1CCC2=CC=C3OCCC3=C12)=O | ||
| 分子式 | C16H21NO3 | 分子量 | 275.34 |
| 溶解度 | DMSO : 100 mg/mL (363.19 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
In vitro comparison of duration of action of melatonin agonists on melatonin MT1 receptor: possible link between duration of action and dissociation rate from receptor
Eur J Pharmacol 2015 Jun 15;757:42-52.PMID:25797281DOI:10.1016/j.ejphar.2015.03.009.
Melatonin MT1 and MT2 receptors are Gi protein-coupled receptors and promising therapeutic targets for a number of diseases. A proportion of G protein-coupled receptor agonists and antagonists have been classified according to their duration of action, which influences their pharmacological efficacy. However, the duration of action of melatonin agonists remains unclear. In this study, we investigated the duration of action of melatonin agonists (melatonin, 2-iodomelatonin, ramelteon, and the Ramelteon metabolite M-II) at the melatonin MT1 receptor, which is more resistant to agonist-induced desensitization than the melatonin MT2 receptor. In Chinese hamster ovary cells stably expressing the human melatonin MT1 receptor, significant differences in the duration of action were observed after 2-h pretreatment with agonists followed by washout. In contrast to melatonin and M-II, the agonist activities of ramelteon and 2-iodomelatonin were persistent (i.e. inhibition of forskolin-stimulated cAMP formation and increase in ERK 1/2 phosphorylation) even after repeated washouts. Similar activities were observed for INS-1 cells endogenously expressing the rat MT1 receptor. Further, we examined potential factors linked to the duration of action. Residual activities of melatonin agonists after washout strongly correlated with their dissociation rates from the human melatonin MT1 receptor, but not their lipophilicity or extent of desensitization. These data suggest that the in vitro duration of action significantly differs between melatonin agonists and might dictate dissociation kinetics. Characterization of these in vitro properties may facilitate further in vivo study of the duration of action.