Diethylmaleate

製品コードS4712 バッチS471202

印刷

化学情報

Chemical Structure Synonyms Diethyl ester, Maleic acid diethyl ester Storage
(From the date of receipt)		 2 years -80°C liquid
化学式

C8H12O4
分子量 172.18 CAS No. 141-05-9
Solubility (25°C)* 体外  
 
 
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

生物活性

製品説明 Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-κB.
in vitro

DEM induces upregulation of GSH(L-c-glutamyl-L-cysteinyl-glycine) metabolism, and the downregulation of pathways of cancer, chemokine signaling, cytokine-cytokine receptor, and focal adhesion in transformed cells. DEM appears to modify microenvironment of transformed cells thereby restraining tumor cell growth. DEM is cytotoxic to the transformed cells in a concentration dependent manner. DEM at 0.25 mM decreases cell viability to 75%. The co-exposure of cells to DEM+GSHe inhibits DEM induced cytotoxicity. DEM exposure increases the ROS generation by multiple orders of magnitude in transformed cells. This is evident from the dose and time dependent increase in fluorescence intensity of CMH2DCFDA. Moreover, DEM activates MAPK pathway and DEM induced activation of ERK is found to be due to phosphorylation at Thr 202/204[1].
in vivo

Sperm motility and epididymal sperm count are significantly reduced in the DEM treated animals. Fertility status is also affected by DEM exposure as is evident from the percent fertility and the litter size. consequences of the oxidative stress produced by the DEM induces glutathione depletion, on the reproductive ability of male mice and modulation of the various components of the antioxidant defense system at the transcriptional level[4].
密度 1.064 g/mL at 25 °C

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Transformed cells (tC3H10T1/2 and tBALB/c)
濃度 Various test concentrations (0.05-1 mM)
反応時間 24 h
実験の流れ

A stock solution of DEM is prepared in 100% DMSO and diluted in DMEM to achieve the desired concentration with less than 0.1% DMSO in the culture wells. Briefly, cells are seeded (1 ×104 cells/well) in 96-well plates and allowed to adhere overnight. Subsequently, these cells are exposed to DEM at various test concentrations (0.05-1 mM) or co-exposed to equimolar (0.25 mM) DEM+GSHe for 24 h. Cell viability is determined by recording the OD at 570 nm in an Elisa microplate reader.
動物実験 動物モデル Sprague-Dawley rats
投薬量 A range of doses up to a maximum of 6mmol/kg
投与方法 i.p

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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