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Dimethyl Fumarate. (Synonyms: 富马酸二甲酯)
目录号: PC11555 纯度: ≥98%
CAS No. :624-49-7
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中文名称
Dimethyl Fumarate.
中文别名
富马酸二甲酯;(E)-2-丁烯二酸二甲酯;反丁烯二酸二甲酯;延胡索酸二甲酯;防霉保鲜剂;霉克星1号;丁烯二酸二甲酯;反-丁烯二酸二甲酯;富马酸二甲酯 标准品;富马酸二甲
英文名称
Dimethyl Fumarate
英文别名
(E)-Dimethyl fumarate;BIS-METHYL ESTER;(E)-2-Butenedioic acid dimethyl ester;FUMARIC ACID DIMETHYL ESTER;TIMTEC-BB SBB008222;2-Butenedioic acid, dimethyl ester, (E)-;2-Butenedioicacid(E)-,dimethylester;Allomaleic acid dimethyl ester;Boletic acid dimethyl ester;Dimethyl (2E)-2-butenedioate;Dimethyl trans-ethylenedicarboxylate;Dimethylester kyseliny fumarove;dimethylester,(e)-2-butenedioicaci;dimethyltrans-butenedioate;Ethylene, 1,2-bis(methoxycarbonyl)-, trans-;Dimethyl fumarate;trans-1,2-Ethylenedicarboxylic Acid;DMF;Tecfidera;Fumaderm;Dimethyl (E)-but-2-enedioate;Fumaric acid, dimethyl ester;Methyl fumarate;trans-Butenedioic acid dimethyl ester;Dimethylfumarate;2-Butenedioic acid (E)-, dimethyl ester;trans-1,2-Ethylenedicarboxylic acid dimethyl ester;BG00012;dimethyl (2E)-but-2-enedioate;BG
Cas No.
624-49-7
分子式
C6H8O4
分子量
144.13
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.

性状

Solid

IC50 & Target[1][2]

Human Endogenous Metabolite

 

体外研究(In Vitro)

Dimethyl fumarate (DMF; 20-200?μM; 24 hours) treatment dose-dependently reduces the viability of SGC-7901, HT29, HCT116 and CT26 cancer cells.
Dimethyl fumarate (DMF; 100?μM; 3-24 hours) significantly activates JNK, p38 and ERK in CT26 cells.
Dimethyl fumarate induces necroptosis in colon cancer cells and the mechanism involves GSH depletion, an increase in ROS and activation of MAPKs-mediated signalling.
Dimethyl fumarate inhibits dendritic cell (DC) maturation by reducing inflammatory cytokine production (IL-12 and IL-6) and the expression of MHC class II, CD80, and CD86. Dimethyl fumarate impairs NF-κB signaling via reduced p65 nuclear translocalization and phosphorylation. Dimethyl fumarate inhibits maturation of DCs and subsequently Th1 and Th17 cell differentiation by suppression of both NF-κB and ERK1/2-MSK1 signaling.
Dimethyl fumarate (DMF), an immune modulator and inducer of the antioxidant response, suppresses HIV replication and neurotoxin release.

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

Cell Viability Assay

Cell Line: SGC-7901, HT29, HCT116 and CT26 cells
Concentration: 20 μM, 50 μM, 100 μM, 200?μM
Incubation Time: 24 hours
Result: Reduced cell viability in SGC-7901, HT29, HCT116 and CT26 cancer cells.

Western Blot Analysis

Cell Line: CT26 cancer cells
Concentration: 100 μM
Incubation Time: 3 hours, 6 hours, 12 hours, 24 hours
Result: Significantly activated JNK, p38 and ERK in CT26 cells after treatment from 3 to 24?h.
体内研究(In Vivo)

Dimethyl fumarate (DMF; 50 mg/kg; oral gavage; daily; for 7 days) treatment is shown to upregulate the mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes, attenuate 6-OHDA induced striatal oxidative stress and inflammation in C57BL/6 mice.

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

Animal Model: Male C57BL/6 mice (8-week-old)
Dosage: 50 mg/kg
Administration: Oral gavage; daily; for 7 days
Result: Was shown to upregulate mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial
结构分类
参考文献
溶解度数据
体外研究: 

DMSO : 50 mg/mL (346.91 mM; Need ultrasonic)

H2O : 8.33 mg/mL (57.80 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.9382 mL 34.6909 mL 69.3818 mL
5 mM 1.3876 mL 6.9382 mL 13.8764 mL
10 mM 0.6938 mL 3.4691 mL 6.9382 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

  • 1.

    建议依照次序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 7.5 mg/mL (52.04 mM); Suspended solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (14.43 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (14.43 mM,饱和度未知) 的澄清溶液。

    以 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 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (14.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 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。

  • 5.

    建议依照次序添加每种溶剂: PBS

    Solubility: 2 mg/mL (13.88 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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