规格 | 价格 | 库存 | 数量 |
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5g |
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25g |
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Other Sizes |
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靶点 |
Microbial Metabolite; Human Endogenous Metabolite
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体外研究 (In Vitro) |
体外活性:褪黑素与剧毒羟基自由基相互作用的速率常数与其他高效羟基自由基清除剂相当。据报道,褪黑激素可以中和过氧化氢、单线态氧、过氧亚硝酸根阴离子、一氧化氮和次氯酸。褪黑激素被认为可以清除剧毒的羟基自由基、过氧亚硝酸根阴离子以及可能的过氧自由基。据报道,褪黑素可以清除超氧阴离子自由基并淬灭单线态氧。褪黑激素刺激超氧化物歧化酶的 mRNA 水平以及谷胱甘肽过氧化物酶、谷胱甘肽还原酶和葡萄糖-6-磷酸脱氢酶(所有这些都是抗氧化酶)的活性,从而提高其抗氧化能力。无细胞系统中的褪黑素已被证明可以直接清除 H2O2、单线态氧 (1O2) 和一氧化氮 (NO*),而在体外很少或没有清除超氧阴离子自由基 (O2*-) 的能力。褪黑激素还可以直接解毒过氧亚硝酸根阴离子 (ONOO-) 和/或过氧亚硝酸 (ONOOH),或该分子的活化形式 ONOOH*。褪黑激素作为直接自由基清除剂,能够解毒活性氧和活性氮。褪黑激素抑制大多数所检查细胞中 cAMP 的积累,但迄今为止,通常仅在一种类型的细胞或组织中观察到吲哚对其他信使的影响。褪黑激素还调节转录因子,即 cAMP 反应元件结合蛋白的磷酸化和 c-Fos 的表达。
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体内研究 (In Vivo) |
褪黑激素增加激活的 PTEN、RSK-1、mTOR 和 AMPKα 激酶的水平,轻度抑制 ERK-1/2 磷酸化和 Bad 磷酸化,显着抑制 S6 核糖体蛋白、4E-BP1、GSK-3α 和 GSK-3β 的磷酸化,以及轻微增加动物体内 PRAS40 磷酸化。褪黑素可改善大脑皮层 Aβ1-42 诱导的神经毒性和星形胶质细胞活化。褪黑激素还可阻止 Aβ1-42 诱导的 Reelin 和 Dab1 表达减少。在小鼠中,褪黑激素治疗和缺乏 NLRP3-/- 对 NF-κB 和 NLRP3 信号通路具有相似的抑制作用。褪黑素治疗和缺乏 NLRP3-/- 具有某些时钟基因表达模式,并改善小鼠心肌细胞形态。
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细胞实验 |
细胞系:HepG2细胞
浓度:1.2 mM 孵育时间:24 h 方法:用不同浓度的药物处理细胞24 h。 |
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动物实验 |
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参考文献 |
分子式 |
C13H16N2O2
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分子量 |
232.28
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精确质量 |
232.12
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元素分析 |
C, 67.22; H, 6.94; N, 12.06; O, 13.78
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CAS号 |
73-31-4
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相关CAS号 |
Melatonin-d4; 66521-38-8; Melatonin-d3; 90735-69-6; Melatonin-d7; 615251-68-8
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外观&性状 |
Solid powder
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SMILES |
CC(=O)NCCC1=CNC2=C1C=C(C=C2)OC
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InChi Key |
DRLFMBDRBRZALE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C13H16N2O2/c1-9(16)14-6-5-10-8-15-13-4-3-11(17-2)7-12(10)13/h3-4,7-8,15H,5-6H2,1-2H3,(H,14,16)
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化学名 |
N-[2-(5-methoxy-1H-indol-3-yl)ethyl]acetamide
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别名 |
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (10.76 mM) (saturation unknown) in 2% DMSO + 40% PEG300 + 5% Tween80 + 53% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (10.76 mM) (saturation unknown) in 2% DMSO 98% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 6: ≥ 1.25 mg/mL (5.38 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 7: ≥ 1.25 mg/mL (5.38 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 8: 5%absolute ethyl alcohol + 95%Corn oil: 2.3mg/ml (9.90mM) 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 4.3051 mL | 21.5257 mL | 43.0515 mL | |
5 mM | 0.8610 mL | 4.3051 mL | 8.6103 mL | |
10 mM | 0.4305 mL | 2.1526 mL | 4.3051 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05257291 | Active Recruiting |
Drug: Melatonin | Essential Hypertension | Azienda Socio Sanitaria Territoriale degli Spedali Civili di Brescia |
February 2, 2018 | Phase 2 |
NCT05654415 | Active Recruiting |
Other: Melatonin Other: Deprivation |
Epilepsy | IRCCS National Neurological Institute "C. Mondino" Foundation |
September 1, 2021 | Not Applicable |
NCT01863446 | Active Recruiting |
Device: Lighting1 Device: Lighting2 |
Pregnancy | Brigham and Women's Hospital | May 2013 | Not Applicable |
NCT00512070 | Active Recruiting |
Drug: olanzapine and melatonin | Schizophrenia Bipolar Disorder Obesity |
Seattle Institute for Biomedical and Clinical Research |
July 2007 | Not Applicable |
NCT05042700 | Active Recruiting |
Drug: Melatonin Drug: Placebo |
Low Anterior Resection Syndrome | Ismail Gögenur | October 13, 2021 | Phase 2 |
Therapeutic effect of melatonin in mouse pups on necrotizing enterocolitis (NEC). Theranostics . 2020 Jun 19;10(17):7730-7746. td> |
Melatonin effects are associated with the lamina propria Th17/Treg balance. Theranostics . 2020 Jun 19;10(17):7730-7746. td> |
Melatonin effects require Th17/Treg balance. Theranostics . 2020 Jun 19;10(17):7730-7746. td> |
Melatonin inhibits cell proliferation. Front Pharmacol . 2022 Sep 26:13:1007006. td> |
Analysis of gene expression changes induced by melatonin. Front Pharmacol . 2022 Sep 26:13:1007006. td> |
Inhibition of gonadotropin-releasing hormone (GnRH)-induced luteinizing hormone (LH) release from neonatal rat gonadotrophs by melatonin. Dispersed cells were attached to culture plates (∼150 000 cells/well) and cultured in 95% air-5% CO2. Physiol Rev . 1998 Jul;78(3):687-721. td> |