1. GPCR/G Protein Neuronal Signaling Autophagy Metabolic Enzyme/Protease Apoptosis
  2. Melatonin Receptor Autophagy Mitophagy Endogenous Metabolite Apoptosis
  3. Melatonin

Melatonin  (Synonyms: 褪黑素; N-Acetyl-5-methoxytryptamine)

目录号: HY-B0075 纯度: 99.93%
COA 产品使用指南

Melatonin 是一种由松果体分泌的激素,可激活褪黑激素受体。Melatonin 在睡眠中起作用并具有重要的抗氧化和抗炎特性。Melatonin 是一种新型的选择性 ATF-6 抑制剂,可通过 COX-2 下调诱导人肝癌细胞凋亡。Melatonin 通过内质网应激减弱palmitic acid-induced (HY-N0830)诱导的小鼠颗粒细胞凋亡。

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Melatonin Chemical Structure

Melatonin Chemical Structure

CAS No. : 73-31-4

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Customer Review

Other Forms of Melatonin:

MCE 顾客使用本产品发表的 88 篇科研文献

WB

    Melatonin purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Oct;22(10):5132-5144.  [Abstract]

    Melatonin regulation of mitophagy activity in the diabetic myocardium, Protein expression with representative gel blots of LC3 I/II, GAPDH (loading control).

    Melatonin purchased from MCE. Usage Cited in: Molecules. 2018 Mar 16;23(3). pii: E675.  [Abstract]

    Representative image of immunobloting of UCP2 in the cultured AC16 cells under various treatments.

    查看 Melatonin Receptor 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress[5].

    IC50 & Target

    Microbial Metabolite

     

    Human Endogenous Metabolite

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    AGS IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    BT-549 IC50
    30 mM
    Compound: Melatonin
    Antiproliferative activity against human BT549 cells after 24 hrs by MTT assay
    Antiproliferative activity against human BT549 cells after 24 hrs by MTT assay
    [PMID: 29144746]
    C6 IC50
    > 40 μM
    Compound: Melatonin
    Antiproliferative activity against rat C6 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against rat C6 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
    [PMID: 34091208]
    CHO EC50
    0.026 nM
    Compound: melatonin
    Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
    Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader
    [PMID: 21568291]
    CHO EC50
    0.069 nM
    Compound: melatonin
    Agonist activity at human melatonin receptor-2 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
    Agonist activity at human melatonin receptor-2 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
    [PMID: 26023814]
    CHO EC50
    0.098 nM
    Compound: melatonin
    Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
    Agonist activity at human melatonin receptor-1 transfected in CHO cell membranes after 1 hr by GTPgammaS binding assay
    [PMID: 26023814]
    CHO EC50
    0.4 nM
    Compound: MLT
    Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr
    Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr
    [PMID: 24417958]
    CHO EC50
    0.49 nM
    Compound: 1
    Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1B
    Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1B
    [PMID: 12646022]
    CHO IC50
    1.1 x 10-10 M
    Compound: Melatonin
    Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
    Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
    [PMID: 27876250]
    CHO EC50
    1.5 nM
    Compound: Melatonin
    Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
    Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
    [PMID: 21420861]
    CHO EC50
    1.7 nM
    Compound: MLT
    Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr
    Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr
    [PMID: 24417958]
    CHO EC50
    2.2 nM
    Compound: MLT
    Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
    Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay
    [PMID: 20444610]
    CHO EC50
    2.24 nM
    Compound: 1
    Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
    Agonist potency determined by [35S]GTP gamma-S binding assay using CHO cell lines for Melatonin receptor type 1A
    [PMID: 12646022]
    CHO-K1 IC50
    0.21 nM
    Compound: melatonin
    Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs
    Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs
    [PMID: 23403082]
    HCT-116 IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    HEK293 EC50
    1 nM
    Compound: Melatonin
    Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
    Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
    [PMID: 31204226]
    HEK293 EC50
    25 nM
    Compound: Melatonin
    Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
    Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay
    [PMID: 31204226]
    HepG2 IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    HepG2 IC50
    271 μM
    Compound: 1, MLT
    Antioxidant activity in human HepG2 cells assessed as reduction in H2O2-induced oxidation by DCFH-DA assay
    Antioxidant activity in human HepG2 cells assessed as reduction in H2O2-induced oxidation by DCFH-DA assay
    [PMID: 23332368]
    HGC-27 IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    MCF7 IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    MCF7 IC50
    18 mM
    Compound: Melatonin
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    [PMID: 29144746]
    MDA-MB-231 IC50
    0.9 μM
    Compound: Melatonin
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    [PMID: 29144746]
    MGC-803 IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    PC-12 IC50
    > 100 μM
    Compound: MLT
    Neuroprotective activity against amyloid beta (25 to 35 amino acid residues) induced damage in rat PC12 cells assessed as cell viability preincubated for 3 hrs followed by addition of amyloid beta (25 to 35 amino acid residues) for 24 hrs by MTT assay
    Neuroprotective activity against amyloid beta (25 to 35 amino acid residues) induced damage in rat PC12 cells assessed as cell viability preincubated for 3 hrs followed by addition of amyloid beta (25 to 35 amino acid residues) for 24 hrs by MTT assay
    [PMID: 26970662]
    SGC-7901 IC50
    > 30 μM
    Compound: Melatonin
    Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 33248852]
    SH-SY5Y EC50
    > 1 μM
    Compound: Melatonin
    Neuroprotective activity against t-BuOOH-induced oxidative stress in human SH-SY5Y cells assessed as inhibition ROS accumulation pre-incubated for 24 hrs before t-BuOOH challnge for 30 mins by DCFH-DA probe based fluorescence assay
    Neuroprotective activity against t-BuOOH-induced oxidative stress in human SH-SY5Y cells assessed as inhibition ROS accumulation pre-incubated for 24 hrs before t-BuOOH challnge for 30 mins by DCFH-DA probe based fluorescence assay
    [PMID: 29420891]
    U-251 IC50
    > 40 μM
    Compound: Melatonin
    Antiproliferative activity against human U-251 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human U-251 cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
    [PMID: 34091208]
    U-87MG ATCC IC50
    > 40 μM
    Compound: Melatonin
    Antiproliferative activity against human U-87 MG cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human U-87 MG cells assessed as growth inhibition incubated for 72 hrs by CCK-8 assay
    [PMID: 34091208]
    体内研究
    (In Vivo)

    褪黑激素增加活化的 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,显著抑制 S6 核糖体蛋白、4E-BP1、GSK-3α 和 GSK-3β 的磷酸化,以及略微增加动物体内的 PRAS40 磷酸化[1]。褪黑激素可改善 Aβ1-42 诱导的大脑皮层神经毒性和星形胶质细胞活化。褪黑激素还可阻断 Aβ1-42[2]诱导的 Reelin 和 Dab1 表达减少。褪黑激素处理和 NLRP3-/- 缺乏对小鼠的 NF-κBNLRP3 信号通路具有相似的抑制作用。褪黑激素处理和 NLRP3-/- 缺乏共享时钟基因表达的一些模式,并改善小鼠心肌细胞形态[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    232.28

    Formula

    C13H16N2O2

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    褪黑素;褪黑激素;美拉酮宁;抑黑素;松果腺素;松果体素

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (430.51 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 12.5 mg/mL (53.81 mM; 超声助溶)

    H2O 中的溶解度 : 1.1 mg/mL (4.74 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 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, 6 months; -20°C, 1 month。-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。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制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

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (10.76 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.76 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制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

      请依序添加每种溶剂: 40% PEG300    60% Saline

      Solubility: 15 mg/mL (64.58 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.93%

    参考文献
    Animal Administration
    [1]

    A total of two sets of adult male C57BL/6j mice weighing 21-26 g are randomly assigned to one of four groups and treated with intraperitoneal (i.p.) delivery of (i) vehicle (50 μL isotonic saline/5% ethanol), (ii) melatonin (4 mg/kg, dissolved in 0.9% isotonic saline/5% ethanol), (iii) Wortmannin, and (iv) melatonin/Wortmannin immediately after reperfusion. In the first set, mice are exposed to 30 min of focal cerebral ischemia (FCI) and 72 h reperfusion for the evaluation of disseminate ischemic injury in the striatum, and signaling pathway analysis (n=7 per group). The second group of mice is exposed to 90 min of FCI and 24 h reperfusion for the analysis of infarct development, brain swelling and IgG extravasation (n=7 per group).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 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, 6 months; -20°C, 1 month。-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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / Ethanol / DMSO 1 mM 4.3051 mL 21.5257 mL 43.0515 mL 107.6287 mL
    Ethanol / DMSO 5 mM 0.8610 mL 4.3051 mL 8.6103 mL 21.5257 mL
    10 mM 0.4305 mL 2.1526 mL 4.3051 mL 10.7629 mL
    15 mM 0.2870 mL 1.4350 mL 2.8701 mL 7.1752 mL
    20 mM 0.2153 mL 1.0763 mL 2.1526 mL 5.3814 mL
    25 mM 0.1722 mL 0.8610 mL 1.7221 mL 4.3051 mL
    30 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
    40 mM 0.1076 mL 0.5381 mL 1.0763 mL 2.6907 mL
    50 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1526 mL
    DMSO 60 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
    80 mM 0.0538 mL 0.2691 mL 0.5381 mL 1.3454 mL
    100 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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