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Monomethyl fumarate
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Monomethyl fumarate
CAS No. : 2756-87-8
MCE 站:Monomethyl fumarate
产品活性:Monomethyl fumarate 是 Dimethyl fumarate (DMF) 的活性代谢产物,一种有效的 GPR109A 激动剂。Monomethyl fumarate 具有用于多种神经保护途径和其他视网膜疾病模型的潜力。
研究领域:GPCR/G Protein | Metabolic Enzyme/Protease
作用靶点:GPR109A | Drug Metabolite
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.
Monomethyl fumarate (25 μM; 24?hours) attenuates 7β-OHC-induced cytotoxicity: cell growth inhibition; decreased cell viability; mitochondrial dysfunction; and cell death induction.
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.
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.
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