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  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)

目錄號: HY-B0075 純度: 99.93%
COA 產(chǎn)品使用指南

Melatonin 是一種由松果體分泌的激素,可激活褪黑激素受體。Melatonin 在睡眠中起作用并具有重要的抗氧化和抗炎特性。Melatonin 是一種新型的選擇性 ATF-6 抑制劑,可通過 COX-2 下調(diào)誘導(dǎo)人肝癌細(xì)胞凋亡。Melatonin 通過內(nèi)質(zhì)網(wǎng)應(yīng)激減弱palmitic acid-induced (HY-N0830)誘導(dǎo)的小鼠顆粒細(xì)胞凋亡。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報,我們不為任何個人用途提供產(chǎn)品和服務(wù)

Melatonin Chemical Structure

Melatonin Chemical Structure

CAS No. : 73-31-4

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10 mM * 1 mL in DMSO ¥500
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500 mg ¥350
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1 g ¥500
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5 g ¥1050
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Customer Review

Other Forms of Melatonin:

MCE 顧客使用本產(chǎn)品發(fā)表的 89 篇科研文獻(xiàn)

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 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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

     

    細(xì)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]
    體內(nèi)研究
    (In Vivo)

    褪黑激素增加活化的 PTEN、RSK-1、mTOR 和 AMPKα 激酶的水平,輕度抑制 ERK-1/2 磷酸化和 Bad 磷酸化,顯著抑制 S6 核糖體蛋白、4E-BP1、GSK-3α 和 GSK-3β 的磷酸化,以及略微增加動物體內(nèi)的 PRAS40 磷酸化[1]。褪黑激素可改善 Aβ1-42 誘導(dǎo)的大腦皮層神經(jīng)毒性和星形膠質(zhì)細(xì)胞活化。褪黑激素還可阻斷 Aβ1-42[2]誘導(dǎo)的 Reelin 和 Dab1 表達(dá)減少。褪黑激素處理和 NLRP3-/- 缺乏對小鼠的 NF-κBNLRP3 信號通路具有相似的抑制作用。褪黑激素處理和 NLRP3-/- 缺乏共享時鐘基因表達(dá)的一些模式,并改善小鼠心肌細(xì)胞形態(tài)[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 號
    性狀

    固體

    顏色

    White to light yellow

    中文名稱

    褪黑素;褪黑激素;美拉酮寧;抑黑素;松果腺素;松果體素

    結(jié)構(gòu)分類
    初始來源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 100 mg/mL (430.51 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

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

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

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請?jiān)?個月內(nèi)使用,-20°C儲存時,請?jiān)?個月內(nèi)使用。

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗(yàn):

    請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

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

    以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑: 40% PEG300    60% Saline

      Solubility: 15 mg/mL (64.58 mM); 澄清溶液; 超聲助溶

    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.93%

    參考文獻(xiàn)
    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.

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請?jiān)?個月內(nèi)使用,-20°C儲存時,請?jiān)?個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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

    * 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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