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Melatonin/褪黑素 {[allProObj[0].p_purity_real_show]}

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。

Melatonin/褪黑素 化学结构 CAS号:73-31-4
Melatonin/褪黑素 化学结构
CAS号:73-31-4
Melatonin/褪黑素 3D分子结构
CAS号:73-31-4
Melatonin/褪黑素 化学结构 CAS号:73-31-4
Melatonin/褪黑素 3D分子结构 CAS号:73-31-4
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Melatonin/褪黑素 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].

Melatonin/褪黑素 细胞实验

Cell Line
Concentration Treated Time Description References
Lithocarpus litseifolius leaf cells 100 µM 14 days Increased accumulation of total flavonoids and dihydrochalcones (including Trilobatin) Int J Mol Sci. 2024 Apr 23;25(9):4592
NP cells 1 mM 24 h Melatonin suppressed NLRP3 inflammasome activation and reduced IL-1β expression Bone Res. 2020 Feb 18;8:10.
ARPE-19 cells 2 mM 24 h Melatonin significantly reduced NaIO3-induced ARPE-19 cell death and inhibited apoptosis and mitochondrial dysfunction. Cell Biosci. 2022 Aug 19;12(1):133.
Mouse oocytes 10μM 12 h To determine whether supplementation of melatonin can ameliorate the quality of maternally aged oocytes in vitro by eliminating the excessive ROS. The results showed that melatonin treatment significantly reduced ROS levels, decreased DNA damage and apoptosis, and restored meiotic defects in aged oocytes. Redox Biol. 2020 Jan;28:101327.
RT7 cells 0, 100, 500, 1000 µM 1 to 17 days To investigate the effect of melatonin on the proliferation of RT7 cells, results showed that melatonin has a cytostatic effect on RT7 cells under normal conditions. Cells. 2023 Aug 30;12(17):2178.
RT7 cells 0, 100, 500, 1000 µM 30 min To investigate the effect of melatonin on the proliferation of RT7 cells after irradiation, results showed that cell proliferation was suppressed in a melatonin concentration-dependent manner. Cells. 2023 Aug 30;12(17):2178.
Endothelial Progenitor Cells (EPCs) 100 μM 4 days Under high glucose conditions, melatonin improved EPC survival, migration, and reduced senescence through AMPK, eNOS, and HO-1 pathways, reversing hyperglycemia-induced oxidative stress. Int J Mol Sci. 2022 Aug 30;23(17):9839.
HCAECs 0.5 mM 6 h Melatonin suppressed cell apoptosis and directly reduced the expression of endothelial cell damage markers in HCAECs. Cell Prolif. 2022 Jun;55(6):e13251.
THP1 cell line 0.5 mM Melatonin decreased the production of pro-inflammatory cytokines in THP1 cell line. Cell Prolif. 2022 Jun;55(6):e13251.
SH-SY5Y human neuroblastoma cells 100 nM 24 h To investigate the effect of melatonin on RA-induced gene expression, results showed that melatonin inhibited RA-induced expression of CYP26A1 and RARB genes. Cells. 2023 Jan 11;12(2):286.
HaCaT cells 1 nM 6-8 h To investigate the effect of melatonin on nNOS expression and NOx production in HaCaT cells. Results showed that 1 nM melatonin significantly increased nNOS mRNA and protein expression and enhanced NOx production within 6-8 h. Int J Mol Sci. 2013 May 28;14(6):11259-76.
Lemna aequinoctialis 10 µM 28 days Investigation of the effect of melatonin on the production of campesterol in Lemna aequinoctialis culture, showing the highest productivity of campesterol (1.79 mg/L). BMC Plant Biol. 2022 Nov 25;22(1):545

Melatonin/褪黑素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice NaIO3-induced retinal degeneration model Oral 25 or 50 mg/kg Once daily for 7 days Melatonin effectively reduced NaIO3-induced retinal injury and repaired the structure of retinal layers. Cell Biosci. 2022 Aug 19;12(1):133.
ICR mice NA/STZ-induced hyperglycemia model Oral 10, 20, 50 mg/kg Once daily for 6 weeks To investigate the effects of different doses of melatonin on glucose homeostasis, antioxidant ability, and adipokine secretion in NA/STZ-induced hyperglycemic mice. Results showed that melatonin could decrease oxidative stress, increase adiponectin levels, and improve dyslipidemia, especially in the high-dose group. Nutrients. 2017 Oct 29;9(11):1187
Mice Aged mouse model Intravenous injection 100 mg/kg Once daily for 10 days To determine whether in vivo supplementation of melatonin can ameliorate the quality of aged oocytes by clearing the excessive ROS. The results showed that melatonin treatment significantly reduced ROS levels, decreased DNA damage and apoptosis, and restored meiotic defects in aged oocytes. Redox Biol. 2020 Jan;28:101327.
ICR mice Radiation-induced oral mucositis model Intraperitoneal and drinking water 100 mg/kg, 50 µg/mL Single intraperitoneal injection, drinking water for 7 days To investigate the preventive effect of melatonin on radiation-induced oral mucositis, results showed that melatonin significantly suppressed radiation-induced oral mucositis. Cells. 2023 Aug 30;12(17):2178.
Mice Streptozotocin (STZ)-induced diabetic mice Intraperitoneal injection 10 mg/kg Daily for 4 weeks Melatonin significantly improved blood flow recovery, EPC mobilization, and capillary density in ischemic hindlimbs of diabetic mice, reducing limb injury. Int J Mol Sci. 2022 Aug 30;23(17):9839.
C57BL/6 mice CAWS-induced KD mouse model Intraperitoneal injection 40 mg/kg Once daily for 30 days Melatonin alleviated vasculitis in the CAWS-induced KD mouse model. Cell Prolif. 2022 Jun;55(6):e13251.
Rats AF puncture-induced IVDD model Intraperitoneal injection 30 mg/kg Weekly, until the day of euthanasia Melatonin alleviated IVDD and LBP by inhibiting NLRP3 inflammasome activation and IL-1β expression Bone Res. 2020 Feb 18;8:10.

Melatonin/褪黑素 动物研究

Dose Mice: 1 mg/kg - 50 mg/kg[4] (i.p.)
Administration i.p.

Melatonin/褪黑素 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 <<

Melatonin/褪黑素 参考文献

[1]Reiter RJ, Tan DX, et al. Actions of melatonin in the reduction of oxidative stress. A review. J Biomed Sci. 2000 Nov-Dec;7(6):444-58.

[2]Reiter RJ. Oxidative damage in the central nervous system: protection by melatonin. Prog Neurobiol. 1998 Oct;56(3):359-84.

[3]Bu LJ, Yu HQ, et al. Melatonin, a novel selective ATF-6 inhibitor, induces human hepatoma cell apoptosis through COX-2 downregulation. World J Gastroenterol. 2017;23(6):986-998.

[4]Bu LJ, Yu HQ, Fan LL, Li XQ, Wang F, Liu JT, Zhong F, Zhang CJ, Wei W, Wang H, Sun GP. Melatonin, a novel selective ATF-6 inhibitor, induces human hepatoma cell apoptosis through COX-2 downregulation. World J Gastroenterol. 2017 Feb 14;23(6):986-998. doi: 10.3748/wjg.v23.i6.986. PMID: 28246472; PMCID: PMC5311108.

[5]Reiter RJ. Oxidative damage in the central nervous system: protection by melatonin. Prog Neurobiol. 1998 Oct;56(3):359-84. doi: 10.1016/s0301-0082(98)00052-5. PMID: 9770244.

Melatonin/褪黑素 实验方案

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

Melatonin/褪黑素 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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
方案 一
方案 二
方案 三
方案 四
方案 五
方案 六
方案 七
配制的工作液建议现用现配,短期内尽快用完。 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
方案 一
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