Dimethyl fumarate (Synonyms:富马酸二甲酯; DMF)
目录号 : KM16236 CAS No. : 624-49-7 纯度 : 98%

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。

规格 价格 是否有货 数量
500mg
In-stock
5g
In-stock
10g 询价 In-stock
50g 询价 In-stock

Other Forms of Rapamycin:

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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.

体外研究

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.

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

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.

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.
分子式
C6H8O4
分子量
144.13
CAS号
624-49-7
中文名称
富马酸二甲酯
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 40 mg/mL (277.53 mM; Need ultrasonic)

配制储备液
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
*

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。

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。

  • 3.

    请依序添加每种溶剂: 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。

  • 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。

临床试验
科研文献
The molarity calculator equation
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