1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  2. Endogenous Metabolite PPAR
  3. Oleoylethanolamide

Oleoylethanolamide  (Synonyms: N-Oleoylethanolamide; Oleamide MEA; Oleic acid monoethanolamide)

目录号: HY-107542 纯度: 99.94%
COA 产品使用指南 技术支持

Oleoylethanolamide 是一种高亲和力的内源性 PPAR-α 激动剂,可用于肥胖和动脉硬化的相关研究。

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Oleoylethanolamide Chemical Structure

Oleoylethanolamide Chemical Structure

CAS No. : 111-58-0

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10 mM * 1 mL in DMSO ¥880
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Other Forms of Oleoylethanolamide:

MCE 顾客使用本产品发表的 1 篇科研文献

查看 PPAR 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.

IC50 & Target[1]

Human Endogenous Metabolite

 

PPAR-α

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
786-0 GI50
35.4 μg/mL
Compound: 4c
Antiproliferative activity against human 786-0 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human 786-0 cells after 48 hrs by sulforhodamine B assay
[PMID: 25510639]
HEK293 EC50
2.2 μM
Compound: OEA
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay
[PMID: 27825553]
HEK293 EC50
2.2 μM
Compound: OEA
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay
[PMID: 28408218]
HEK293 EC50
2.2 μM
Compound: OEA
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
Agonist activity at human GPR119 expressed in HEK293 cells assessed as cAMP accumulation after 60 mins
[PMID: 23357035]
HEK293 EC50
2200 nM
Compound: OEA
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine
[PMID: 23374864]
HeLa EC50
0.12 μM
Compound: OEA
Transactivation of human Gal4 fused PPARalpha LBD transfected in human HeLa cells after 7 hrs by dual-luciferase reporter gene assay
Transactivation of human Gal4 fused PPARalpha LBD transfected in human HeLa cells after 7 hrs by dual-luciferase reporter gene assay
[PMID: 27622746]
HeLa EC50
1.1 μM
Compound: OEA
Transactivation of human Gal4 fused PPARdelta LBD transfected in human HeLa cells after 7 hrs by dual-luciferase reporter gene assay
Transactivation of human Gal4 fused PPARdelta LBD transfected in human HeLa cells after 7 hrs by dual-luciferase reporter gene assay
[PMID: 27622746]
MCF7 EC50
152 nM
Compound: OEA
Agonist activity at human PPARalpha transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
Agonist activity at human PPARalpha transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
[PMID: 26226490]
MCF7 EC50
152 nM
Compound: OEA
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay
[PMID: 24936232]
MCF7 EC50
185 nM
Compound: OEA
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay
[PMID: 24936232]
MCF7 GI50
25.9 μg/mL
Compound: 4c
Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay
[PMID: 25510639]
NCI/ADR-RES GI50
9.1 μg/mL
Compound: 4c
Antiproliferative activity against human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay
[PMID: 25510639]
NCI-H460 GI50
36.5 μg/mL
Compound: 4c
Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
[PMID: 25510639]
OVCAR-3 GI50
35.4 μg/mL
Compound: 4c
Antiproliferative activity against human OVCAR3 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human OVCAR3 cells after 48 hrs by sulforhodamine B assay
[PMID: 25510639]
PC-3 GI50
16.9 μg/mL
Compound: 4c
Antiproliferative activity against human PC3 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human PC3 cells after 48 hrs by sulforhodamine B assay
[PMID: 25510639]
RBL-2H3 IC50
> 50 μM
Compound: 10
Antiallergic activity in rat RBL2H3 cells assessed as inhibition of DNP-HSA-mediated degranulation by measuring decrease in beta-hexosaminidase activity preincubated for 30 mins followed by DNP-HSA stimulation and measured after 30 mins by 4-nitrophenyl 2
Antiallergic activity in rat RBL2H3 cells assessed as inhibition of DNP-HSA-mediated degranulation by measuring decrease in beta-hexosaminidase activity preincubated for 30 mins followed by DNP-HSA stimulation and measured after 30 mins by 4-nitrophenyl 2
[PMID: 31618024]
SK-OV-3 IC50
24 μM
Compound: N-oleylethanolamine
Inhibition of ceramidase in human SKOV3 cells assessed as hydrolysis of N-((2S,3R)-1,3-dihydroxy-5-((2-oxo-2H-chromen-7- yl)oxy)pentan-2-yl)palmitamide at 16 uM after 24 hrs at 37 degC by HPLC
Inhibition of ceramidase in human SKOV3 cells assessed as hydrolysis of N-((2S,3R)-1,3-dihydroxy-5-((2-oxo-2H-chromen-7- yl)oxy)pentan-2-yl)palmitamide at 16 uM after 24 hrs at 37 degC by HPLC
[PMID: 20085856]
SK-OV-3 IC50
28 μM
Compound: N-oleylethanolamine
Inhibition of ceramidase in human SKOV3 cells assessed as hydrolysis of N-((2S,3R)-1,3-dihydroxy-5-((2-oxo-2H-chromen-7- yl)oxy)pentan-2-yl)palmitamide at 16 uM after 24 hrs at 37 degC by umbelliferone formation based fluorescence intensity assay
Inhibition of ceramidase in human SKOV3 cells assessed as hydrolysis of N-((2S,3R)-1,3-dihydroxy-5-((2-oxo-2H-chromen-7- yl)oxy)pentan-2-yl)palmitamide at 16 uM after 24 hrs at 37 degC by umbelliferone formation based fluorescence intensity assay
[PMID: 20085856]
U-251 GI50
27.3 μg/mL
Compound: 4c
Antiproliferative activity against human U251 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human U251 cells after 48 hrs by sulforhodamine B assay
[PMID: 25510639]
体外研究
(In Vitro)

油酰乙醇胺 (OEA) 是一种内源性 PPAR-α 配体,可减轻靶向肝星状细胞的肝纤维化。Oleoylethanolamide 通过 PPAR-α 在体外抑制 TGF-β1 诱导的肝星状细胞 (HSC) 活化。为了评估油酰乙醇胺对 HSC 活化的影响,通过 qPCR 检查了 TGF-β1 刺激的 HSC 中 α-SMA 和 Col1a 的表达水平。在用 TGF-β1 (5 ng/mL) 刺激 48 小时的 CFSC 细胞组中,α-SMA 和 Col1a 的 mRNA 水平被显著诱导,而当用油酰乙醇胺处理时,mRNA 水平以剂量依赖性方式被抑制。免疫荧光和蛋白质印迹结果表明,油酰乙醇胺抑制剂量依赖性地抑制 α-SMA 的蛋白质表达,α-SMA 是 HSC 活化的标志物。Oleoylethanolamide 对 HSC 活化的抑制作用被 PPAR-α 拮抗剂 MK886 (10 μM) 完全阻断。此外,PPAR-α 的 mRNA 和蛋白质表达水平在 TGF-β1 刺激下下调,而油酰乙醇胺处理以剂量依赖性方式恢复这些变化。此外,在 TGF-β1 刺激存在的情况下,Smad 2/3 的磷酸化被上调,这与观察到的对 HSC 活化的影响一致,而油酰乙醇胺 (10 μM) 降低了用 TGF-β1 模拟的 CFSC 中 Smad2/3 的磷酸化[1]

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

体内研究
(In Vivo)

油酰乙醇胺 (OEA) 可显著抑制肝纤维化小鼠模型中促纤维化细胞因子 TGF-β1 负调节 TGF-β1 信号通路 (α-SMA、胶原蛋白 1a 和胶原蛋白 3a) 中的基因。油酰乙醇胺 (5 mg/kg/天,腹膜内注射,腹膜内注射) 通过阻断肝星状细胞 (HSC) 的活化,显著减缓两种实验动物模型的肝纤维化进程[1] .

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

Clinical Trial
分子量

325.53

Formula

C20H39NO2

CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 20.83 mg/mL (63.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0719 mL 15.3596 mL 30.7191 mL
5 mM 0.6144 mL 3.0719 mL 6.1438 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.39 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.39 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.94%

参考文献
Cell Assay
[1]

CFSC, HSC cell lines are first obtained from cirrhotic rat liver, and have a similar phenotype to that of early passage primary HSCs. CFSC cells are cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. All cells are cultured in 6-well culture plates under 37°C and 5% CO2 in an incubator. The medium is replaced every two days, and the cells are harvested and diluted at a ratio of 1:3 twice a week. In experiments, HSCs are pretreated with the experimental concentration of Oleoylethanolamide (30 μM, 10 μM, 3 μM) before stimulation with 5 ng/mL TGF-β1. mRNA expression levels of α-SMA (A) and Col1a (B) are analyzed by real-time PCR[1].

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

Animal Administration
[1]

Mice[1]
The Sv/129 mice and PPAR-α knockout mice are maintained in a room with controlled temperature (21-23°C), humidity (55-60%) and lighting (12 h light/dark cycles) and given water ad libitum. Mice are randomly divided for methionine choline-deficient (MCD) and thioacetamide (TAA) experiments. In the MCD-diet feeding experiment, wild-type Sv/129 mice and PPAR-α knockout mice are each divided into three groups (n=8 /group): (i) control group receive normal diet; (ii) fed with MCD diet and injected with the vehicle (5% Tween-80+5% PEG400+90% saline, 5 mL/kg/day, 8 weeks, intraperitoneal injection, i.p.); (iii) fed with MCD diet along with Oleoylethanolamide administration (5 mg/kg/day; 8 weeks, i.p.). In another set of experiment, all the wild-type mice and PPAR-α knockout mice are given standard chow diet, and are randomly separated into three groups: the control group is not administrated TAA or Oleoylethanolamide but is injected with the saline; the TAA group is injected with TAA (160 mg/kg, three times per week, 6 weeks, dissolved in saline, i.p.) plus the corresponding vehicle; the Oleoylethanolamide group is both injected with TAA and Oleoylethanolamide (5 mg/kg/day; 6 weeks, i.p.)[1].

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

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0719 mL 15.3596 mL 30.7191 mL 76.7978 mL
5 mM 0.6144 mL 3.0719 mL 6.1438 mL 15.3596 mL
10 mM 0.3072 mL 1.5360 mL 3.0719 mL 7.6798 mL
15 mM 0.2048 mL 1.0240 mL 2.0479 mL 5.1199 mL
20 mM 0.1536 mL 0.7680 mL 1.5360 mL 3.8399 mL
25 mM 0.1229 mL 0.6144 mL 1.2288 mL 3.0719 mL
30 mM 0.1024 mL 0.5120 mL 1.0240 mL 2.5599 mL
40 mM 0.0768 mL 0.3840 mL 0.7680 mL 1.9199 mL
50 mM 0.0614 mL 0.3072 mL 0.6144 mL 1.5360 mL
60 mM 0.0512 mL 0.2560 mL 0.5120 mL 1.2800 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Oleoylethanolamide
目录号:
HY-107542
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