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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,可誘導抗氧化劑基因表達上調。Dimethyl fumarate 通過 GSH 耗竭/ROS 升高/MAPKs 激huo途徑誘導結腸癌細胞壞死,并誘導細胞自噬 (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:624-49-7
中文名稱:富馬酸二甲酯
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數據
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 |
請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內使用,-20°C 儲存時,請在 1 個月內使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結果的可靠性,澄清的儲備液可以根據儲存條件,適當保存;體內實驗的工作液,建議您現用現配,當天使用; 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沉淀、析出現象,可以通過加熱和/或超聲的方式助溶
請依序添加每種溶劑: 50% PEG300 50% saline
Solubility: 7.5 mg/mL (52.04 mM); Suspended solution; Need ultrasonic
參考文獻
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,可誘導抗氧化劑基因表達上調。Dimethyl fumarate 通過 GSH 耗竭/ROS 升高/MAPKs 激huo途徑誘導結腸癌細胞壞死,并誘導細胞自噬 (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:624-49-7
中文名稱:富馬酸二甲酯
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數據
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 |
請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內使用,-20°C 儲存時,請在 1 個月內使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結果的可靠性,澄清的儲備液可以根據儲存條件,適當保存;體內實驗的工作液,建議您現用現配,當天使用; 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沉淀、析出現象,可以通過加熱和/或超聲的方式助溶
請依序添加每種溶劑: 50% PEG300 50% saline
Solubility: 7.5 mg/mL (52.04 mM); Suspended solution; Need ultrasonic
參考文獻