Luteolin

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

目录号：S2320 Purity: 99.18%

Luteolin (Luteoline, Luteolol, Digitoflavone)是一种非选择性的PDE抑制剂，作用于PDE1-5，K_i分别为15.0 μM， 6.4 μM， 13.9 μM， 11.1 μM和9.5 μM。

Luteolin Chemical Structure

CAS: 491-70-3

规格	价格	库存
10mM (1mL in DMSO)	RMB 790	现货
10mg	RMB 630.63	现货
50mg	RMB 1417.78	现货
200mg	RMB 4686.02	现货
1g	RMB 12039.3	现货
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客户使用Selleck的Luteolin发表文献24篇

客户使用该产品的1个实验数据

产品质控

批次：纯度： 99.18%

99.18

Luteolin相关产品

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ADC Cytotoxin抑制剂选择性比较

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PDE1-5，K_i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]

参考文献
[1] Yu MC, et al. Eur J Pharmacol, 2010, 627(1-3), 269-275. [2] Xagorari A, et al. J Pharmacol Exp Ther, 2001, 296(1), 181-187.

参考文献

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
Smiles	C1=CC(=C(C=C1C2=CC(=O)C3=C(C=C(C=C3O2)O)O)O)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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

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
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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，注：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：取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：取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.

C1=C0/X	C1:	LOG(C1):
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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):