Luteolin

别名: Luteoline, Luteolol, Digitoflavone 中文名称:木犀草素,四羟黄酮

Luteolin (Luteoline, Luteolol, Digitoflavone)是一种非选择性的PDE抑制剂,作用于PDE1-5Ki分别为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

规格 价格 库存 购买数量
10mM (1mL in DMSO) 790 现货
10mg 630.63 现货
50mg 1417.78 现货
200mg 4686.02 现货
1g 12039.3 现货
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Luteolin相关产品

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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 23786520
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 25190466
HL60 cells Proliferation assay 30 μM 48 h Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay 18258440
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 25176187
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 23411073
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 24955889
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 24900447
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 20932762
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 24900447
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 23411073
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 21275386
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 8158164
mouse B16-4A5 cells Function assay 72 h Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs, IC50=14 μM 20189399
K562 cells Growth inhibition assay 5 days Growth inhibition of K562 cells by XTT assay after 5 days, IC50=14.65 μM 17411092
human H9 cells Cytotoxicity assay 3 days Cytotoxicity against human H9 cells after 3 days, IC50=16 μM 8158164
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 24900447
human U937 cells Proliferation assay 72 h Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=20 μM 17158054
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 24245939
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 20731357
CHO cells Function assay Agonist activity at rat DAT expressed in CHO cells, EC50=1.45 μM 20971650
RBL-2H3 cells Function assay Inhibitory activity against IL-4 production in RBL-2H3 cells was determined, IC50=3.7 μM 12951092
human mast cells Function assay Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=4.5 μM 22257213
human LNCAP cells Function assay Downregulation of prostate specific antigen secretion in human LNCAP cells, IC50=5 μM 25019478
MDCK cells Cytotoxicity assay Cytotoxicity against MDCK cells by MTT assay, CC50=12.44 μM 18640042
点击查看更多细胞系数据

生物活性

产品描述 Luteolin (Luteoline, Luteolol, Digitoflavone)是一种非选择性的PDE抑制剂,作用于PDE1-5Ki分别为15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM和9.5 μM。
靶点
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)
体外研究(In Vitro)
体外研究活性

Luteolin是在诃子中发现的黄酮类化合物,是非选择性的磷酸二酯酶PDE抑制剂,对PDE1-5的Ki值分别为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的产生,IC50值低于1 μM。Luteolin抑制LPS诱导的Akt和IkappaBalpha的磷酸化。[2]

实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性

LD50:小鼠>2500毫克/千克(i.g.) [3]

化学信息&溶解度

分子量 286.24 分子式

C15H10O6

CAS号 491-70-3 SDF Download Luteolin SDF
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 57 mg/mL ( (199.13 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 20 mg/mL (69.87 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 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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