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富马酸单甲酯

富马酸单甲酯用途

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。

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富马酸单甲酯名称

[ CAS 号 ]:
2756-87-8

[ 中文名 ]:
富马酸单甲酯

[ 英文名 ]:
Monomethyl fumarate

[英文别名 ]:

MFCD00063174
(2E)-4-Methoxy-4-oxobut-2-enoic acid
2-Butenedioic acid, monomethyl ester, (2E)-
EINECS 220-412-6
(2E)-4-Methoxy-4-oxo-2-butenoic acid
Methyl Hydrogen Fumarate
2-Butenedioic acid, monomethyl ester
Monomethyl Fumarate
4-Methoxy-4-oxobut-2-enoic acid
Fumaric acid, monomethyl ester

富马酸单甲酯生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> GPR109A

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

[体外研究]

富马酸单乙酯抑制forskolin诱导的cAMP合成,IC50为70nm。富马酸单甲酯诱导9.4μM的EC50转染GPR109A细胞产生剂量依赖性Ca2+信号[1]。富马酸单乙酯(25μM；24 h)可减弱7β-OHC诱导的细胞毒性：细胞生长抑制；细胞活力下降；线粒体功能障碍；细胞死亡诱导[3]。

[体内研究]

光照前单剂量富马酸单甲酯(50-100 mg/kg；IP)以剂量依赖的方式防止这些形态学变化(强光照射导致感光细胞死亡)[2]。富马酸单乙酯(100毫克/千克)可减少视网膜炎症和氧化应激。富马酸单甲酯显著抑制NFkB途径中的光诱导视网膜病变(LIR)上调基因,包括：Nlrp3、Casp1、Il-1β和Tnf-α[2]。动物模型：白化BALB/c小鼠(雄性,6周龄)[2]剂量：50、65、75、100mg/kg给药：IP结果：以剂量依赖的方式阻止了这些形态学改变(强光照射引起的光感受器死亡)。

[参考文献]

[1]. Tang H, et al. The psoriasis drug monomethylfumarate is a potent nicotinic acid receptor agonist. Biochem Biophys Res Commun. 2008 Oct 31;375(4):562-5.

[2]. Jiang D, et al. Monomethyl Fumarate Protects the Retina From Light-Induced Retinopathy. Invest Ophthalmol Vis Sci. 2019 Mar 1;60(4):1275-1285.

[3]. Sghaier R, et al. Dimethyl fumarate and monomethyl fumarate attenuate oxidative stress and mitochondrialalterations leading to oxiapoptophagy in 158N murine oligodendrocytes treated with 7β-hydroxycholesterol. J Steroid Biochem Mol Biol. 2019 Nov;194:105432.

富马酸单甲酯物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
250.0±23.0 °C at 760 mmHg

[ 熔点 ]:
144-145ºC

[ 分子式 ]:
C₅H₆O₄

[ 分子量 ]:
130.099

[ 闪点 ]:
108.9±16.1 °C

[ 精确质量 ]:
130.026611

[ PSA ]:
63.60000

[ LogP ]:
-0.24

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.469

[ 储存条件 ]:
室温，干燥

富马酸单甲酯MSDS

详细MSDS(安全技术说明书)

富马酸单甲酯安全信息

[ 符号 ]:

GHS05

[ 信号词 ]:
Danger

[ 危害声明 ]:
H318

[ 警示性声明 ]:
P280-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi:Irritant;

[ 风险声明 (欧洲) ]:
R41

[ 安全声明 (欧洲) ]:
S26-S39

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ 海关编码 ]:
2918990090

富马酸单甲酯合成路线

详细合成路线

富马酸单甲酯上下游产品

富马酸单甲酯上游产品

富马酸单甲酯下游产品

富马酸单甲酯海关

[ 海关编码 ]: 2918990090

[ 中文概述 ]:
2918990090. 其他含其他附加含氧基羧酸（包括酸酐、酰卤化物、过氧化物和过氧酸及该税号的衍生物）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2918990090. other carboxylic acids with additional oxygen function and their anhydrides, halides, peroxides and peroxyacids; their halogenated, sulphonated, nitrated or nitrosated derivatives. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

富马酸单甲酯文献

Altered Oligodendrocyte Maturation and Myelin Maintenance: The Role of Antiretrovirals in HIV-Associated Neurocognitive Disorders.

J. Neuropathol. Exp. Neurol. 74 , 1093-118, (2015)

Despite effective viral suppression through combined antiretroviral therapy (cART), approximately half of HIV-positive individuals have HIV-associated neurocognitive disorders (HAND). Studies of antir...

Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).

Bioorg. Med. Chem. Lett. 21 , 2736-9, (2011)

Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids ...

Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway.

Br. J. Pharmacol. 172 , 3929-43, (2015)

Dimethyl fumarate (DMF) is a newly approved drug for the treatment of relapsing forms of multiple sclerosis and relapsing-remitting multiple sclerosis. Here, we investigated the effects of DMF and its...

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