富马酸单甲酯

生物活性靶点体外研究体内研究富马酸单甲酯试剂级价格

富马酸单甲酯

CAS号:2756-87-8
英文名:Monomethyl fumarate
中文名:富马酸单甲酯
CBNumber:CB7505423
分子式:C5H6O4
分子量:130.1
MOL File:2756-87-8.mol

富马酸单甲酯化学性质

熔点 :144-145 °C (lit.)
沸点 :250.0±23.0 °C(Predicted)
密度 :1.37 g/cm3
储存条件 :2-8°C
溶解度 :Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
酸度系数(pKa) :3.40±0.10(Predicted)
形态 :Solid
颜色 :Off-White
最大波长(λmax) :209nm(MeOH)(lit.)
CAS 数据库 :2756-87-8(CAS DataBase Reference)

安全信息

危险品标志 :Xi
危险类别码 :41
安全说明 :26-39
WGK Germany :3
海关编码 :29171900

富马酸单甲酯性质、用途与生产工艺

生物活性 Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate) 是牛皮癣药物Fumaderm的活性代谢产物，是一种有效的 GPR109A 的激动剂。Monomethyl Fumarate 可预防与神经退行性疾病相关的主要功能障碍：氧化应激、线粒体功能障碍、凋亡和自噬。
靶点
Target Value
GPR109A
()
体外研究

Monomethyl fumarate completely inhibits forskolin induced cAMP synthesis with an IC ₅₀ of 70 nM. Monomethyl fumarate induces a dose-dependent Ca ²⁺ signal in GPR109A transfected cells with an EC ₅₀ 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.