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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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