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

Monomethyl fumarate 

Cat. No.: HY-103252 Purity: 97.67%
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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10 mM * 1 mL in DMSO USD 55 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (768.64 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 7.6864 mL 38.4320 mL 76.8639 mL
5 mM 1.5373 mL 7.6864 mL 15.3728 mL
10 mM 0.7686 mL 3.8432 mL 7.6864 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 97.67%

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Keywords:

MonomethylGPR109ADrug MetaboliteHM74APUMA-GHCA2HCAR2 metaboliteDimethylfumarateDMFneuroprotectiveretinalInhibitorinhibitorinhibit

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Product Name:
Monomethyl fumarate
Cat. No.:
HY-103252
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