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  1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis Autophagy
  2. ROR Reactive Oxygen Species Apoptosis Autophagy
  3. Nobiletin

Nobiletin  (Synonyms: 川陳皮素)

目錄號: HY-N0155 純度: 99.79%
COA 產品使用指南

Nobiletin 是一種來自柑橘皮的聚甲氧基黃酮,可改善記憶力喪失,是一種 RORs 激動劑。Nobiletin 可以降低分化的 C2C12 肌管中的 ROS 的水平,并具有抗炎和抗癌特性,包括抗血管生成,抗增殖,抗轉移和誘導細胞凋亡。

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

Nobiletin Chemical Structure

Nobiletin Chemical Structure

CAS No. : 478-01-3

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10 mM * 1 mL in DMSO ¥825
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1 mg ¥340
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5 mg ¥750
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10 mg ¥1100
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50 mg ¥3300
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100 mg ¥5100
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1 g   詢價  

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Customer Review

Other Forms of Nobiletin:

    Nobiletin purchased from MCE. Usage Cited in: Nutrients. 2023 Apr 7, 15(8), 1801.

    Nobiletin (Nob; 100 mg/kg/day; s.c.; 10 weeks) markedly reduces D-gal (D-galactose)-induced increases in the ratio of p-FOXO 3a/FOXO and the expression of MAFbx and MuRF1 in mice.

    查看 ROR 亞型特異性產品:

    • 生物活性

    • 純度 & 產品資料

    • 參考文獻

    生物活性

    Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis[1][2][3][4].

    IC50 & Target

    Retinoid acid receptor-related orphan receptors (RORs)[1]; reactive oxygen species (ROS)[1]; apoptosis[2]

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CWR22R IC50
    36.53 μM
    Compound: 44
    Antiproliferative activity against human 22Rv1 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human 22Rv1 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    DU-145 IC50
    144.5 μM
    Compound: 44
    Antiproliferative activity against human DU-145 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human DU-145 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    HL-60 IC50
    10 ng/mL
    Compound: Nobiletin
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    [PMID: 31398616]
    HL-60 IC50
    41.5 μM
    Compound: I
    Antiproliferative activity against HL60 after 24 hrs
    Antiproliferative activity against HL60 after 24 hrs
    [PMID: 17391969]
    HT-29 IC50
    24 μM
    Compound: 4, Nobiletin
    Anticancer activity against human HT-29 cells after 72 hrs by MTT assay
    Anticancer activity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 19054677]
    LNCaP C4-2 IC50
    30.3 μM
    Compound: 44
    Antiproliferative activity against human C4-2 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human C4-2 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    MCF7 IC50
    4.4 μM
    Compound: 20
    Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
    Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
    [PMID: 21354800]
    MDCK IC50
    4.9 μM
    Compound: 20
    Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
    Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
    [PMID: 21354800]
    Monocyte IC50
    10 μM
    Compound: Nobiletin
    Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
    Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
    [PMID: 10096854]
    PC-3 IC50
    122.6 μM
    Compound: 44
    Antiproliferative activity against human PC-3 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human PC-3 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    體外研究
    (In Vitro)

    Nobiletin (0-100 μM;24 小時;U2OS 和 HOS 細胞) 處理逐漸降低 MMP-2MMP-9 的蛋白表達。在 U2OS 和 HOS 細胞中,Nobiletin 顯著降低 p-IKKα/β 和 p-IκBα 的磷酸化,以及細胞核部分中 NF-κB 的蛋白表達,同時增加胞質部分中的 NF-κB 表達。Nobiletin 下調細胞核中p-CREB 和SP-1 的表達,而Nobiletin 不影響c-Jun 和c-Fos 的表達[1]。
    Nobiletin (0-100 μM;24 小時;U2OS 和 HOS 細胞) 處理顯著降低 U2OS 和 HOS 細胞中 MMP-2MMP-9mRNA 表達,且呈劑量依賴性[1]。

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

    Western Blot Analysis[1]

    Cell Line: U2OS and HOS cells
    Concentration: 0 μM, 25 μM, 50 μM, 75 μM, 100 μM
    Incubation Time: 24 hours
    Result: Progressively reduced protein expressions of MMP-2 and MMP-9. Considerably reduced the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Down-regulated the p-CREB and the SP-1 expressions in the nuclear fraction in U2OS and HOS cells.

    RT-PCR[1]

    Cell Line: U2OS and HOS cells
    Concentration: 0 μM, 25 μM, 50 μM, 75 μM, 100 μM
    Incubation Time: 24 hours
    Result: Significantly reduced mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells.
    體內研究
    (In Vivo)

    Nobiletin (常規(guī)飲食的 0.1%;口服給藥;每天;持續(xù) 20 周;雄性 C57BL/6 小鼠) 處理可恢復老年小鼠的葡萄糖穩(wěn)態(tài)并促進能量消耗和晝夜節(jié)律活動[2]。

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

    Animal Model: 20- to 22-month-old male C57BL/6 mice[2]
    Dosage: 0.1% of regular diet
    Administration: Oral administration; daily; for 20 weeks
    Result: Fully restored glucose tolerance in aged mice, and increased basal body temperature and cold tolerance in aged mice. Led to a twofold increase in distance run/day on voluntary wheels compared with aged regular diet-fed mice during the active phase.
    分子量

    402.39

    Formula

    C21H22O8

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    蜜橘黃素;川皮亭;川皮苷;川陳皮素

    結構分類
    初始來源
    運輸條件

    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 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 50 mg/mL (124.26 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質量 1 mg 5 mg 10 mg
    1 mM 2.4852 mL 12.4258 mL 24.8515 mL
    5 mM 0.4970 mL 2.4852 mL 4.9703 mL
    查看完整儲備液配制表

    * 請根據(jù)產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,避免反復凍融造成的產品失效
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內使用, -20°C儲存時,請在6個月內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    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

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?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:
    ——為保證實驗結果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.21 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。
    • 方案 二

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

      Solubility: ≥ 2.08 mg/mL (5.17 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.8 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。
    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    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

    由于實驗過程有損耗,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 網站選購。 ,Tween 80,均可在 MCE 網站選購。
    計算結果
    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品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術支持聯(lián)系。
    動物實驗體內工作液的配制方法 : 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 & 產品資料

    純度: 99.79%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產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,避免反復凍融造成的產品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內使用, -20°C儲存時,請在6個月內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4852 mL 12.4258 mL 24.8515 mL 62.1288 mL
    5 mM 0.4970 mL 2.4852 mL 4.9703 mL 12.4258 mL
    10 mM 0.2485 mL 1.2426 mL 2.4852 mL 6.2129 mL
    15 mM 0.1657 mL 0.8284 mL 1.6568 mL 4.1419 mL
    20 mM 0.1243 mL 0.6213 mL 1.2426 mL 3.1064 mL
    25 mM 0.0994 mL 0.4970 mL 0.9941 mL 2.4852 mL
    30 mM 0.0828 mL 0.4142 mL 0.8284 mL 2.0710 mL
    40 mM 0.0621 mL 0.3106 mL 0.6213 mL 1.5532 mL
    50 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2426 mL
    60 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0355 mL
    80 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7766 mL
    100 mM 0.0249 mL 0.1243 mL 0.2485 mL 0.6213 mL
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    目錄號:
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