产品说明书
Melatonin
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同义名 : | 松果体素 ;N-Acetyl-5-methoxytryptamine;NSC 56423;5-Methoxy-N-acetyltryptamine;Circadin;Melatonine;Regulin;NSC 113928 |
| CAS号 : | 73-31-4 | |
| 货号 : | A204285 | |
| 分子式 : | C13H16N2O2 | |
| 纯度 : | 97% | |
| 分子量 : | 232.28 | |
| MDL号 : | MFCD00005655 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(452.04 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 1 mg/mL(4.31 mM)，配合低频超声助溶 无水乙醇: 12 mg/mL(51.66 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Activating transcription factor 6 (ATF-6) is one of the three main endoplasmic reticulum(ER) transmembrane sensors that elicit the unfolded protein response(UPR). Melatonin (N-acetyl-5-methoxytryptamine), produced in the human pineal gland during the night phase of the light-dark cycle, plays important roles in physiological and pharmacological functions and also acts as a novel selective ATF-6 inhibitor. Melatonin treatment (10-5 mM) for 24 h after pretreatment by tunicamycin inhibited the expression COX-2 by downregulating ATF-6, which increased the apoptosis of HepG2 cells via CHOP and Bcl-2/Bax pathway[4]. Melatonin was an effective free radical scavenger and antioxidant which reduced amyloid β protein toxicity of Alzheimer’s disease, reduced oxidative damage in several models of Parkinson’s disease, protected against glutamate excitotoxicity, reduced ischemia-reperfusion injury, lowered neural damage due to d-aminolevulinic acid (phorphyria), hyperbaric hyperoxia and a variety of neural toxins. It also had been shown to reduce lipid peroxidation and oxidative damage to nuclear DNA[5]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| CHO cells | Function assay | Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells, Ki=8.00E-05 μM | 9435890 | ||
| CHO-Galpha16 cells | Function assay | 20 mins | Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.56 nM | 21237644 | |
| CHOK1 | Function assay | 3 h | Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, IC50=0.21 nM | 23403082 | |
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00869128 | Diabetes Mellitus, Type 2 ... 展开 >> Insomnia 收起 << | Phase 2 | Completed | - | - |
| NCT00869128 | - | Completed | - | - | |
| NCT02500017 | Night-eating Syndrome | Not Applicable | Terminated(Difficulty recruiti... 展开 >>ng appropriate participants) 收起 << | - | United States, Connecticut ... 展开 >> Connecticut Mental Health Center New Haven, Connecticut, United States, 06519 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
4.31mL 0.86mL 0.43mL |
21.53mL 4.31mL 2.15mL |
43.05mL 8.61mL 4.31mL |
| 参考文献 |
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