1. GPCR/G Protein
    Metabolic Enzyme/Protease
  2. GPR109A
    Drug Metabolite
  3. Monomethyl fumarate

Monomethyl fumarate 

Cat. No.: HY-103252
Handling Instructions

Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.

For research use only. We do not sell to patients.

Monomethyl fumarate Chemical Structure

Monomethyl fumarate Chemical Structure

CAS No. : 2756-87-8

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Description

Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease[1][2][3].

In Vitro

Monomethyl fumarate completely inhibits forskolin induced cAMP synthesis with an IC50 of 70 nM. Monomethyl fumarate induces a dose-dependent Ca2+ signal in GPR109A transfected cells with an EC50 of 9.4 μM[1].
Monomethyl fumarate (25 μM; 24 hours) attenuates 7β-OHC-induced cytotoxicity: cell growth inhibition; decreased cell viability; mitochondrial dysfunction; and cell death induction[3].

In Vivo

A single dose of Monomethyl fumarate (50-100 mg/kg; IP) before light exposure prevents these morphologic changes (bright light exposure induced photoreceptor death) in a dose-dependent manner[2].
Monomethyl fumarate (100 mg/kg) reduces retinal inflammation and oxidative stress. Monomethyl fumarate significantly suppresses light-induced retinopathy (LIR) upregulated genes in the NFkB pathway including: Nlrp3, Casp1, Il-1β, and Tnf-α[2].

Animal Model: Albino BALB/c mice (male, 6 weeks old)[2]
Dosage: 50, 65, 75, 100 mg/kg
Administration: IP
Result: Prevented these morphologic changes (bright light exposure induced photoreceptor death) in a dose-dependent manner.
Molecular Weight

130.10

Formula

C₅H₆O₄

CAS No.

2756-87-8

SMILES

O=C(OC)/C=C/C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

MonomethylGPR109ADrug MetaboliteHM74APUMA-GHCA2HCAR2 metaboliteDimethylfumarateDMFneuroprotectiveretinalInhibitorinhibitorinhibit

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Monomethyl fumarate
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