An active metabolite of dimethyl fumarate; an agonist of HCA2/GPR109A (EC50 = 9.4 µM); reduces neutrophil adhesion to endothelial cells stimulated with TNF

Monomethyl fumarate – 100 g

Brand:
Cayman
CAS:
2756-87-8
Storage:
-20
UN-No:
Non-Hazardous - /

Monomethyl fumarate is an active metabolite of the immune modulator dimethyl fumarate (Item No. 14714) that is rapidly formed from dimethyl fumarate by hydrolysis.{46318} It is an agonist of the hydroxycarboxylic acid 2 (HCA2) receptor/GPR109A with an EC50 value of 9.4 µM for inducing calcium accumulation in CHO cells expressing the receptor.{46319} Monomethyl fumarate reduces neutrophil adhesion to endothelial cells stimulated with TNF, decreases CXCL2-directed neutrophil migration, and increases the expression of the Nrf2 target gene NQO1 in wild-type but not HCA2-/- macrophages.{46320} It inhibits proliferation and induces differentiation in keratinocytes, as well as decreases the levels of TNF-α induced by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) in keratinocytes when used at a concentration of 1 mM.{46321} Monomethyl fumarate (1 mg/day) reduces symptoms of experimental autoimmune encephalomyelitis (EAE) in mice and isolated natural killer cells from these mice induced cytotoxicity in previously isolated immature and mature dendritic cells.{46322} Formulations containing monomethyl fumarate have been used in the treatment of multiple sclerosis.  

 

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SKU: 27813 - 100 g Category:

Description

An active metabolite of dimethyl fumarate; an agonist of HCA2/GPR109A (EC50 = 9.4 µM); reduces neutrophil adhesion to endothelial cells stimulated with TNF, decreases CXCL2-directed neutrophil migration, and increases the expression of the Nrf2 target gene NQO1 in wild-type but not HCA2-/- macrophages; inhibits proliferation and induces differentiation in keratinocytes, as well as decreases TPA-induced levels of TNF-α in keratinocytes at 1 mM; reduces symptoms of EAE in mice at 1 mg/day

Formal name: 2E-butenedioic acid, 1-methyl ester

Synonyms:  Fumaric acid, monomethyl ester

Molecular weight: 130.1

CAS: 2756-87-8

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience

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