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.
体外研究
Monomethyl fumarate completely inhibits forskolin induced cAMP synthesis with an IC50 of 70 nM. Monomethyl fumarate induces a dose-dependent Ca signal in GPR109A transfected cells with an EC50 of 9.4 μM.
Monomethyl fumarate (25 μM; 24 hours) attenuates 7β-OHC-induced cytotoxicity: cell growth inhibition; decreased cell viability; mitochondrial dysfunction; and cell death induction.
体内研究
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.
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.
Animal Model:
Albino BALB/c mice (male, 6 weeks old)
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.
分子式
C5H6O4
分子量
130.10
CAS号
2756-87-8
中文名称
富马酸单甲酯
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 100 mg/mL (768.64 mM; Need ultrasonic)
H2O : 10 mg/mL (76.86 mM; ultrasonic and warming and heat to 60°C)