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Dimethyl fumarate

Catalog No. T0492   CAS 624-49-7
Synonyms: DMF

Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.

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Dimethyl fumarate Chemical Structure
Dimethyl fumarate, CAS 624-49-7
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Purity: 90.51%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.
In vitro PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl2, 0.5 μM cAMP or cGMP, and [3H]cAMP or [3H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration[3].
In vivo Dimethyl fumarate inhibits nuclear entry of NF-kappaB in RHEC and reduces myocardial infarct size after ischemia and reperfusion in rats in vivo. [3] Dimethyl fumarate oral administration is shown to upregulate mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes, attenuate 6-OHDA induced striatal oxidative stress and inflammation in C57BL/6 mice. [5]
Synonyms DMF
Molecular Weight 144.13
Formula C6H8O4
CAS No. 624-49-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 14.4 mg/mL (100 mM)

Ethanol: 7.2 mg/mL (50 mM)

TargetMolReferences and Literature

1. Albrecht P, et al. J Neuroinflammation,2012, 9, 163. 2. Peng H, et al. J Biol Chem,2012, 287(33), 282017-28026. 3. Meili-Butz S, et al. Eur J Pharmacol,2008, 586(1-3), 251-258. 4. Cross SA, et al. J Immunol,2011, 187(10), 52015-5025. 5. Jing X, et al. Neuroscience,2015, 286, 131-140. 6. Li Y, et al. Dimethyl fumarate accelerates wound healing under diabetic condition. J Mol Endocrinol. 2018 Jul 23. pii: JME-18-0102. 7. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors[J]. European Journal of Medicinal Chemistry. 2020: 113030.

TargetMolCitations

1. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. European Journal of Medicinal Chemistry,. 2021 Feb 15;212:113030

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library EMA Approved Drug Library Anti-Neurodegenerative Disease Compound Library Drug-Fragment Library NO PAINS Compound Library Bioactive Compounds Library Max Covalent Inhibitor Library

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Keywords

Dimethyl fumarate 624-49-7 Autophagy Immunology/Inflammation Metabolism Microbiology/Virology NF-Κb Proteases/Proteasome Reactive Oxygen Species Nrf2 Endogenous Metabolite HIV Protease Antioxidant neuroprotective Dimethyl Inhibitor Keap1-Nrf2 inhibit anti-inflammatory DMF Dimethyl Fumarate brain-penetrant ROS Human immunodeficiency virus sclerosis HIV inhibitor

 

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