Dimethyl fumarate (富馬酸二甲酯)

Dimethyl fumarate (DMF) 是一種具有口服活性且可透過(guò)血腦屏障的 Nrf2 激活劑，可誘導(dǎo)抗氧化劑基因表達(dá)上調(diào)。Dimethyl fumarate 通過(guò) GSH 耗竭/ROS 升高/MAPKs 激活途徑誘導(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。貨號(hào)：HY-17363 ，CAS：624-49-7

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號(hào)：HY-17363

起訂量：1

規(guī)格:：500mg

價(jià)格:：￥400

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產(chǎn)品詳情

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(guò)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(guò) 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(chēng)：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)

配制儲(chǔ)備液

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。

In Vivo:

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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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

Dimethyl fumarate (富馬酸二甲酯)

Dimethyl fumarate (DMF) 是一種具有口服活性且可透過(guò)血腦屏障的 Nrf2 激活劑，可誘導(dǎo)抗氧化劑基因表達(dá)上調(diào)。Dimethyl fumarate 通過(guò) GSH 耗竭/ROS 升高/MAPKs 激活途徑誘導(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。貨號(hào)：HY-17363 ，CAS：624-49-7

品牌：MCE

型號(hào)：HY-17363

起訂量：1

規(guī)格:：500mg

價(jià)格:：￥400

15906629305

在線客服

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產(chǎn)品詳情

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(guò)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(guò) 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(chēng)：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)

配制儲(chǔ)備液

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。

In Vivo:

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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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

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Dimethyl fumarate (Synonyms: 富馬酸二甲酯)

Dimethyl fumarate (富馬酸二甲酯)

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Dimethyl fumarate (Synonyms: 富馬酸二甲酯)