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別名: NSC 76751, Hexamethoxyflavone 中文名稱:蜜橘黃素,川陳皮素
Nobiletin是O-甲基黃酮,是從柑橘果皮如橘子分離的一種黃酮類化合物。具有抗炎和抗腫瘤活性。
Nobiletin Chemical Structure
CAS: 478-01-3
相關(guān)靶點 | MMP1 MMP2 MMP3 MMP7 MMP8 MMP9 MMP12 MMP13 MMP14 MMP26 | 點擊展開 |
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相關(guān)產(chǎn)品 | Ilomastat (GM6001) Batimastat (BB-94) SB-3CT Marimastat (BB-2516) T-5224 NSC 405020 MMP-9-IN-1 JNJ0966 Cordycepin 1, 10-Phenanthroline monohydrate o-Phenanthroline Lactobionic acid CL-82198 Auraptene | 點擊展開 |
相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 蛋白酶抑制劑庫 泛素化化合物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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SHSY5Y | Function assay | 30 uM | 3 hrs | Elevation of phosphorylated ERK level in hydrogen peroxide-treated human SHSY5Y cells at 30 uM after 3 hrs by Western blot analysis | 18282757 |
SHSY5Y | Function assay | 30 uM | 3 hrs | Elevation of phosphorylated p38 level in hydrogen peroxide-treated human SHSY5Y cells at 30 uM after 3 hrs by Western blot analysis | 18282757 |
SHSY5Y | Function assay | 30 uM | 3 hrs | Elevation of phosphorylated JNk level in hydrogen peroxide-treated human SHSY5Y cells at 30 uM after 3 hrs by Western blot analysis | 18282757 |
ST-13 | Function assay | 10 uM | 11 days | Induction of preadipocyte differentiation in mouse ST-13 cells assessed as lipid accumulation at 10 uM within 11 days by oil red-staining relative to control | 19268587 |
ST-13 | Function assay | 0.1 to 30 uM | 11 days | Induction of adipocyte differentiation in mouse ST-13 cells assessed as stimulation of adipsin mRNA expression at 0.1 to 30 uM within 11 days by semi-quantitative RT-PCR | 19268587 |
ST-13 | Function assay | 0.1 to 30 uM | 11 days | Induction of adipocyte differentiation in mouse ST-13 cells assessed as stimulation of adipocyte P2 mRNA expression at 0.1 to 30 uM within 11 days by semi-quantitative RT-PCR | 19268587 |
SRA 01/04 | Growth inhibition assay | 64 uM | 4 days | Growth inhibition of human SRA 01/04 cells assessed as reduction in PCNA expression at 64 uM after 4 days by Western blot analysis | 23199882 |
SRA 01/04 | Function assay | 24 hrs | Inhibition of TNF-alpha-induced proMMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE analysis, IC50=17μM | 21723726 | |
SRA 01/04 | Function assay | 24 hrs | Inhibition of TNFalpha-stimulated pro MMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE based gelatin zymography assay, IC50=17μM | 22047798 | |
SRA 01/04 | Function assay | 24 hrs | Inhibition of PMA-induced proMMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE analysis, IC50=20.9μM | 21723726 | |
SRA 01/04 | Function assay | 24 hrs | Inhibition of PMA-stimulated pro MMP9 production in human SRA 01/04 cells after 24 hrs by SDS-PAGE based gelatin zymography assay, IC50=20.9μM | 22047798 | |
HT-29 | Anticancer assay | 72 hrs | Anticancer activity against human HT-29 cells after 72 hrs by MTT assay, IC50=24μM | 19054677 | |
SHSY5Y | Function assay | 12 hrs | Reduction of hydrogen peroxide-induced apoptotic cell death in human SHSY5Y cells assessed as DNA ladder formation after 12 hrs | 18282757 | |
ST-13 | Function assay | 11 days | Induction of adipocyte differentiation in mouse ST-13 cells assessed as increase in PPARgamma2 mRNA level after 11 days by semi-quantitative RT-PCR relative to control | 19268587 | |
MCF-7 MX | Function assay | Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=4.4μM | 21354800 | ||
MDCK | Function assay | Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=4.9μM | 21354800 | ||
NIH-3T3-G185 | Function assay | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50=11.5μM | 11743742 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Nobiletin是O-甲基黃酮,是從柑橘果皮如橘子分離的一種黃酮類化合物。具有抗炎和抗腫瘤活性。 | |
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Nobiletin,從柑橘果皮,如橘子中分離得到的柑橘黃酮,具有抗炎和抗腫瘤活性。Nobiletin,一個聚甲氧基黃酮,能夠抑制NO和O 2-的產(chǎn)生。Nobiletin顯著抑制使用雙倍TPA引起的皮膚炎癥。它也會抑制環(huán)氧合酶-2的表達,以及誘導型NO合酶蛋白和前列腺素E2的釋放。[1]在人工基底膜模型中,Nobiletin抑制人類纖維肉瘤HT-1080細胞的腫瘤侵襲活性,不僅通過抑制MMPs的表達,也通過妨礙磷脂酰肌醇3-激酶途徑(PI3-K)增加TIMP-1的產(chǎn)生來發(fā)揮作用。[2] Nobiletin可能也會通過抑制巨噬細胞海綿狀細胞的形成而防止血管壁水平的動脈粥樣硬化。[3] |
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體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | LD50: 780毫克/千克(i.g.). [4] |
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分子量 | 402.39 | 分子式 | C21H22O8 |
CAS號 | 478-01-3 | SDF | Download Nobiletin SDF |
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 80 mg/mL ( (198.81 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Ethanol : 3 mg/mL (7.45 mM) Water : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
澄清溶液 |
5%DMSO
Corn oil
|
1.0mg/ml (2.49mM) | 以 1 mL 工作液為例,取50μL20mg/ml的澄清DMSO儲備液加到950μL玉米油中,混合均勻。工作液請現(xiàn)配現(xiàn)用! | ||
澄清溶液 |
5%DMSO
40%
5%
50%ddH2O
|
4.0mg/ml (9.94mM) | 以 1 mL 工作液為例,取50μL80mg/ml的澄清DMSO儲備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用! |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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