货号:A204285
同义名:
松果体素
/ N-Acetyl-5-methoxytryptamine; NSC 56423
Melatonin是一种由松果体分泌的激素,能调节睡眠周期,具有抗氧化、抗炎作用,同时是一种 ATF-6 抑制剂,能够下调 COX-2,增强线粒体自噬并调节凋亡和自噬的稳态。
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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]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 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 | |
HEK293 cells | Function assay | Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.2 nM | 11063602 | ||
Dose | Mice: 1 mg/kg - 50 mg/kg[4] (i.p.) |
Administration | i.p. |
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 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
4.31mL 0.86mL 0.43mL |
21.53mL 4.31mL 2.15mL |
43.05mL 8.61mL 4.31mL |
CAS号 | 73-31-4 |
分子式 | C13H16N2O2 |
分子量 | 232.28 |
SMILES Code | COC1=CC2=C(NC=C2CCNC(C)=O)C=C1 |
MDL No. | MFCD00005655 |
别名 | 松果体素 ;N-Acetyl-5-methoxytryptamine; NSC 56423; 5-Methoxy-N-acetyltryptamine; Circadin; Melatonine; Regulin; NSC 113928 |
运输 | 蓝冰 |
InChI Key | DRLFMBDRBRZALE-UHFFFAOYSA-N |
Pubchem ID | 896 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的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
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