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    • Luteolin

      別名: Luteoline, Luteolol, Digitoflavone 中文名稱:木犀草素,四羥黃酮

      Luteolin (Luteoline, Luteolol, Digitoflavone)是一種非選擇性的PDE抑制劑,作用于PDE1-5Ki分別為15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM和9.5 μM。

      Luteolin Chemical Structure

      Luteolin Chemical Structure

      CAS: 491-70-3

      規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
      10mM (1mL in DMSO) 790 現(xiàn)貨
      10mg 630.63 現(xiàn)貨
      50mg 1417.78 現(xiàn)貨
      200mg 4686.02 現(xiàn)貨
      1g 12039.3 現(xiàn)貨
      更大包裝 有超大折扣

      400-668-6834

      [email protected]

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      細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

      細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息(PMID)
      human THP1 cells Function assay 20 μM 1 h Downregulation of TPA-induced NOX2 mRNA expression in human THP1 cells at 20 uM incubated for 1 hr prior to TPA challenge measured after 24 hrs by RT-PCR analysis
      MDA-MB-231 cells Function assay 5 μM 16 h Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay
      HL60 cells Proliferation assay 30 μM 48 h Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay
      mouse RAW264.7 cells Function assay 2 h Inhibition of NO production in LPS-stimulated mouse RAW264.7 cells pre-incubated for 2 hrs before LPS stimulation for 24 hrs by Griess assay method, IC50=0.21 μM
      human MV4-11 cells Cytotoxicity assay 72 h Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=1.76 μM
      HEK293 cells Function assay 24 h Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=2.3 μM
      human U2OS cells Function assay 5 h Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay, EC50=3.2 μM
      rat H9c2 cells Function assay 24 h Cytoprotective activity against doxorubicin-induced cytotoxicity in rat H9c2 cells assessed as cell viability after 24 hrs by MTT assay, EC50=5.53 μM
      human HT-29 cells Function assay 10 mins Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay, EC50=7.24 μM
      human RS4:11 cells Cytotoxicity assay 72 h Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=7.25 μM
      NCI-H460 cells Function assay 2-20 h Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation after 2 to 20 hrs relative to fumitremorgin C, IC50=8.9 μM
      human H9 cells Function assay 3 days Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=10 μM
      mouse B16-4A5 cells Function assay 72 h Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs, IC50=14 μM
      K562 cells Growth inhibition assay 5 days Growth inhibition of K562 cells by XTT assay after 5 days, IC50=14.65 μM
      human H9 cells Cytotoxicity assay 3 days Cytotoxicity against human H9 cells after 3 days, IC50=16 μM
      human HT-29 cells Function assay 10 mins Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins, IC50=18.6 μM
      human U937 cells Proliferation assay 72 h Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=20 μM
      mouse HT22 cells Function assay 3 h Neuroprotective activity in mouse HT22 cells assessed as t-BOOH-induced toxicity at 40 uM preincubated for 3 hrs followed by t-BOOH induction measured after 9 hrs by MTT assay
      HEK293 FS cells Function assay Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=0.85 μM
      CHO cells Function assay Agonist activity at rat DAT expressed in CHO cells, EC50=1.45 μM
      RBL-2H3 cells Function assay Inhibitory activity against IL-4 production in RBL-2H3 cells was determined, IC50=3.7 μM
      human mast cells Function assay Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=4.5 μM
      human LNCAP cells Function assay Downregulation of prostate specific antigen secretion in human LNCAP cells, IC50=5 μM
      MDCK cells Cytotoxicity assay Cytotoxicity against MDCK cells by MTT assay, CC50=12.44 μM
      點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

      生物活性

      產(chǎn)品描述 Luteolin (Luteoline, Luteolol, Digitoflavone)是一種非選擇性的PDE抑制劑,作用于PDE1-5Ki分別為15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM和9.5 μM。
      靶點(diǎn)
      PDE2 [1]
      (Cell-free assay)
      PDE5 [1]
      (Cell-free assay)
      PDE4 [1]
      (Cell-free assay)
      PDE3 [1]
      (Cell-free assay)
      PDE1 [1]
      (Cell-free assay)
      6.4 μM(Ki) 9.5 μM(Ki) 11.1 μM(Ki) 13.9 μM(Ki) 15.0 μM(Ki)
      體外研究(In Vitro)
      體外研究活性

      Luteolin是在訶子中發(fā)現(xiàn)的黃酮類化合物,是非選擇性的磷酸二酯酶PDE抑制劑,對(duì)PDE1-5的Ki值分別為15.0 μM,6.4 μM,13.9 μM,11.1 μM以及9.5 μM。[1] Luteolin抑制LPS刺激的TNF-α的產(chǎn)生,IC50值低于1 μM。Luteolin抑制LPS誘導(dǎo)的Akt和IkappaBalpha的磷酸化。[2]

      實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
      Western blot FADD / PARP / Cleaved PARP Caspase-3 / Cleaved Caspase-3 / Caspase-8 / Cleaved Caspase-8 ERK / p-ERK / JNK / p-JNK / p38 / p-p38 / Bax / Bcl-2 p-VEGFR2 / p-mTOR / pS6K1 / p70S6K1 / pAKT / AKT / MMP-2 / MMP-9 p21 / Survivin / Cyclin D1 DNMT1 / DMNT3A / DNMT3B TET1 / TET2 / TET3 30992674
      Immunofluorescence 5-hmC 30988303
      Growth inhibition assay Cell viability 30992674
      體內(nèi)研究(In Vivo)
      體內(nèi)研究活性

      LD50:小鼠>2500毫克/千克(i.g.) [3]

      • https://pubmed.ncbi.nlm.nih.gov/19853596/
      • https://pubmed.ncbi.nlm.nih.gov/11123379/

      化學(xué)信息&溶解度

      分子量 286.24 分子式

      C15H10O6

      CAS號(hào) 491-70-3 SDF Download Luteolin SDF
      儲(chǔ)存條件(自收到貨起)

      體外溶解度
      批次:

      DMSO : 57 mg/mL ( (199.13 mM) ;DMSO吸濕會(huì)降低化合物溶解度,請(qǐng)使用新開(kāi)封DMSO)

      Ethanol : 20 mg/mL (69.87 mM)

      Water : Insoluble

      摩爾濃度計(jì)算器

      體內(nèi)溶解配方
      批次:

      現(xiàn)配現(xiàn)用,請(qǐng)按從左到右的順序依次添加,澄清后再加入下一溶劑

      動(dòng)物體內(nèi)配方計(jì)算器

      實(shí)驗(yàn)計(jì)算

      摩爾濃度計(jì)算器

      質(zhì)量 濃度 體積 分子量

      動(dòng)物體內(nèi)配方計(jì)算器(澄清溶液)

      第一步:請(qǐng)輸入基本實(shí)驗(yàn)信息(考慮到實(shí)驗(yàn)過(guò)程中的損耗,建議多配一只動(dòng)物的藥量)

      mg/kg g μL

      第二步:請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方)

      % DMSO % % Tween 80 % ddH2O
      %DMSO %

      計(jì)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,:如該濃度超過(guò)該批次藥物DMSO溶解度,請(qǐng)先聯(lián)系Selleck);

      體內(nèi)配方配制方法: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: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(jìn)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。

      技術(shù)支持

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      操作手冊(cè)

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      常見(jiàn)問(wèn)題及建議解決方法

      問(wèn)題 1:
      Would you please suggest a suitable vehicle to dissolve Luteolin for in vivo i.p. use?

      回答:
      Formula: 5% DMSO+40% PEG 300+5% Tween80+ddH2O, working Solution concentration: up to 7.5mg/ml, stable for 30min.

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