双氯芬酸二乙胺 T0432

Product Introduction
Bioactivity


英文名: Diclofenac diethylamine

描述: Diclofenac diethylamine 是非选择性抗炎剂，通过活化 caspase 级联反应来诱导神经干细胞凋亡。它是一种COX 抑制剂，在 CHO 细胞中，对人COX-1和COX-2的IC50值分别为 4 和 1.3 nM。它对绵羊COX-1和COX-2的IC50值分别为 5.1 μM 和0.84 μM。

激酶实验: HDAC Activity: HDAC activity is measured using a continuous trypsin-coupled assay. For inhibitor characterization, measurements are done in a reaction volume of 100 μL using 96-well assay plates. For each isozyme, the HDAC protein in reaction buffer [50 mM HEPES, 100 mM KCl, 0.001% Tween 20, 5% DMSO (pH 7.4), supplemented with bovine serum albumin at concentrations of 0% (HDAC1), 0.01% (HDAC2, 3, 8, and 10), or 0.05% (HDAC6)] is mixed with PCI-24781 at various concentrations and allowed to incubate for 15 minutes. Trypsin is added to a final concentration of 50 nM, and acetyl-Gly-Ala-(N-acetyl-Lys)-AMC is added to a final concentration of 25 μM (HDAC1, 3, and 6), 50 μM (HDAC2 and 10), or 100 μM (HDAC8) to initiate the reaction. Negative control reactions are done in the absence of PCI-24781 in replicates of eight. Reactions are monitored in a fluorescence plate reader. After a 30-minute lag time, the fluorescence is measured over a 30-minute time frame using an excitation wavelength of 355 nm and a detection wavelength of 460 nm. The increase in fluorescence with time is used as the measure of the reaction rate. Inhibition constants Ki(app) are obtained using the program BatchKi.

体外活性: Diclofenac diethylamine 通过抑制环氧合酶（COX）来阻断前列腺素的合成来发挥其抗炎、解热和镇痛的作用。此外，Diclofenac diethylamine 通过抑制细菌DNA的合成表现出抗菌活性。Diclofenac diethylamine 的副作用是抑制COX，减少胃上皮的前列腺素，使胃更易受到胃酸的腐蚀。Diclofenac diethylamine 对 COX2-同工酶有从低到中等的选择性抑制作用（大约10倍）。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 69 mg/mL (186.8 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 55 mg/mL (148.93 mM)


关键字: Cyclooxygenase | anti-inflammatory | cascade | CHO | COX-1 | neural | Inhibitor | NSCs | stem | ovine | caspase | inhibit | COX | Diclofenac diethylamine | cells | Apoptosis | COX-2 | Diclofenac

相关产品: Hexamethonium Bromide | Raddeanin A | Glaucocalyxin A | PP5-IN-1 | BX-912 | Umbelliferone | iCRT-5 | PI-103 | Amentoflavone | AOH1996

相关库: Anti-Aging Compound Library | FDA-Approved Drug Library | Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compound Library

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