Size | Price | Stock | Qty |
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500mg |
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1g |
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5g |
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Other Sizes |
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Purity: ≥98%
Dimethyl Fumarate (DMF, trade names Tecfidera; Skilarence), the methyl ester of fumaric acid, is a potent, orally bioactive and brain-penetrant immunomodulator and Nrf2 activator. It has been approved by the U.S. FDA for the treatment of relapsing multiple sclerosis and by the European Medicines Agency (EMA) for managing moderate-to-severe plaque psoriasis.
Targets |
Nrf2
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ln Vitro |
Dimethyl fumarate (DMF; 20–200 μM; 24 hours) significantly lowers SGC-7901, HT29, HCT116, and CT26 viability [1]. In CT26 cells, dimethyl fumarate (DMF; 100 μM; 3–24 hours) dramatically activates p38, ERK, and JNK[1]. By decreasing inflammatory transduction pathways involving GSH depletion, raising ROS, and stimulating MAPK-mediated signaling, dimethyl fumarate acts [1]. By lowering the expression of MHC class II, CD80, and CD86, as well as the synthesis of inflammatory cytokines (IL-12 and IL-6), dimethyl fumarate prevents dendritic cell (DC) development. Dimethyl fumarate reduces DC maturation and cumulative Th1 and Th17 cell secretion by blocking NF-κB and ERK1/2-MSK1 signaling. Dimethyl fumarate also impairs p65 nuclear translocation and phosphorylation [2]. Dimethyl fumarate (DMF), an immunological antioxidant response cell viability assay [1]
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ln Vivo |
Dimethyl fumarate (DMF; 50 mg/kg; daily; for 7 days) administration was demonstrated to upregulate Nrf2-regulated cytoprotective genes' mRNA and protein levels and to reduce 6-OHDA-induced C57BL striae. Eight-week-old male C57BL/6 mice serve as an animal model for body oxidation [4].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: SGC-7901, HT29, HCT116 and CT26 Cell Tested Concentrations: 20 μM, 50 μM, 100 μM, 200 μM incubation Modulators and inducers, inhibiting HIV replication and neurotoxin release [3]. Incubation Duration: 24 hrs (hours) Experimental Results: diminished cell viability in SGC-7901, HT29, HCT116 and CT26 cancer cells. Western Blot Analysis [1] Cell Types: CT26 cancer cells Tested Concentrations: 100 μM Incubation Duration: 3 hrs (hours), 6 hrs (hours), 12 hrs (hours), 24 hrs (hours) Experimental Results: JNK, p38 and ERK were Dramatically activated in CT26 cells after 3 to 24 hrs (hours) of treatment . |
Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (8weeks old)[4]
Doses: 50 mg/kg Route of Administration: po (oral gavage); daily; for 7 days Experimental Results:Was shown to upregulate mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes. |
References |
[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 |
Molecular Formula |
C6H8O4
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Molecular Weight |
144.12
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Exact Mass |
144.0423
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Elemental Analysis |
C, 50.00; H, 5.60; O, 44.40
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CAS # |
624-49-7
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Related CAS # |
Dimethyl fumarate-d6;66487-95-4;Dimethyl fumarate-d2;23057-98-9
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Appearance |
White to off-white solid
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Source |
Endogenous Metabolite
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LogP |
0.7
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tPSA |
52.6Ų
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SMILES |
O=C(OC)/C=C/C(OC)=O
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InChi Key |
LDCRTTXIJACKKU-ONEGZZNKSA-N
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InChi Code |
InChI=1S/C6H8O4/c1-9-5(7)3-4-6(8)10-2/h3-4H,1-2H3/b4-3+
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Chemical Name |
But-2-enedioic acid dimethyl ester
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Synonyms |
DMF Dimethylfumarate Dimethyl Fumarate
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~41.67 mg/mL (~289.11 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (14.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (14.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (14.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (13.88 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). Solubility in Formulation 5: 7.5 mg/mL (52.04 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 6.9387 mL | 34.6933 mL | 69.3866 mL | |
5 mM | 1.3877 mL | 6.9387 mL | 13.8773 mL | |
10 mM | 0.6939 mL | 3.4693 mL | 6.9387 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.