Dimethyl fumarate (Synonyms: 富馬酸二甲酯)
Dimethyl fumarate (DMF) 是一種具有口服活性且可透過血腦屏障的 Nrf2 激huo劑，可誘導(dǎo)抗氧化劑基因表達(dá)上調(diào)。Dimethyl fumarate 通過 GSH 耗竭/ROS 升高/MAPKs 激huo途徑誘導(dǎo)結(jié)腸癌細(xì)胞壞死，并誘導(dǎo)細(xì)胞自噬 (autophagy)。Dimethyl fumarate 可用于多發(fā)性硬化癥的研究。
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
IC50 & Target：Human Endogenous Metabolite
體外研究(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 releas
| 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. |
體內(nèi)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
| 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. |
分子量：144.13
Formula：C6H8O4
CAS 號(hào)：624-49-7
中文名稱：富馬酸二甲酯
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式：
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 62.5 mg/mL (433.64 mM; Need ultrasonic)
H2O : 8.33 mg/mL (57.80 mM; ultrasonic and warming and heat to 60°C)
| 濃度溶劑體積質(zhì)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 |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請(qǐng)依序添加每種溶劑： 50% PEG300 50% saline
Solubility: 7.5 mg/mL (52.04 mM); Suspended solution; Need ultrasonic
- 2.
請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution
- 3.
請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution
4.請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution
參考文獻(xiàn)
[1]. Xin Xie, et al. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway. Br J Pharmacol. 2015 Aug;172(15):3929-43.
[2]. Peng H, et al. Dimethyl fumarate inhibits dendritic cell maturation via nuclear factor κB (NF-κB) and extracellular signal-regulated kinase 1 and 2 (ERK1/2) and mitogen stress-activated kinase 1 (MSK1) signaling. J Biol Chem. 2012 Aug 10;287(33):28017-26.
[3]. Cross SA, et al. Dimethyl fumarate, an immune modulator and inducer of the antioxidant response, suppresses HIV replication and macrophage-mediated neurotoxicity: a novel candidate for HIV neuroprotection. J Immunol. 2011 Nov 15;187(10):5015-25.
[4]. Jing X, et al. Dimethyl fumarate attenuates 6-OHDA-induced neurotoxicity in SH-SY5Y cells and in animal model of Parkinson's disease by enhancing Nrf2 activity. Neuroscience. 2015 Feb 12;286:131-40
注：產(chǎn)品僅用于科研
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