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Dimethyl Fumarate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dimethyl Fumarate图片
CAS NO:624-49-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
500mg电议
5 g电议
10 g电议
50 g电议

产品名称
富马酸二甲酯
产品介绍
Dimethyl fumarate (DMF) 是一种具有口服活性且可透过血脑屏障的Nrf2激活剂,可诱导抗氧化剂基因表达上调。Dimethyl fumarate 通过 GSH 耗竭/ROS升高/MAPKs 激活途径诱导结肠癌细胞坏死,并诱导细胞自噬 (autophagy)。Dimethyl fumarate 可用于多发性硬化症的研究。
生物活性

Dimethyl fumarate (DMF) is an orally active and brain-penetrantNrf2activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate inducesnecroptosisin coloncancercells through GSH depletion/ROSincrease/MAPKs activation pathway, and also induces cellautophagy. Dimethyl fumarate can be used for multiple sclerosis research[1][2].

IC50& Target

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[1].
Dimethyl fumarate (DMF; 100 μM; 3-24 hours) significantly activates JNK, p38 and ERK in CT26 cells[1].
Dimethyl fumarate induces necroptosis in colon cancer cells and the mechanism involves GSH depletion, an increase in ROS and activation of MAPKs-mediated signalling[1].
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[2].
Dimethyl fumarate (DMF), an immune modulator and inducer of the antioxidant response, suppresses HIV replication and neurotoxin release[3].

Cell Viability Assay[1]

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[1]

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[4].

Animal Model:Male C57BL/6 mice (8-week-old)[4]
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.
Clinical Trial
分子量

144.13

性状

Solid

Formula

C6H8O4

CAS 号

624-49-7

中文名称

富马酸二甲酯

结构分类
  • Others
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM6.9382 mL34.6909 mL69.3818 mL
5 mM1.3876 mL6.9382 mL13.8764 mL
10 mM0.6938 mL3.4691 mL6.9382 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 50%PEG300   50% saline

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

  • 2.

    请依序添加每种溶剂: 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 ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 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.

    请依序添加每种溶剂: 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.

    请依序添加每种溶剂: PBS

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

*以上所有助溶剂都可在本网站选购。