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Inotilone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Inotilone图片
CAS NO:906366-79-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
cyclooxygenase (COX) inhibitor
Cas No.906366-79-8
别名(2E)-2-[(3,4-二羟基苯基)亚甲基]-5-甲基-3(2H)-呋喃酮
化学名(2Z)-2-[(3,4-dihydroxyphenyl)methylene]-5-methyl-3(2H)-furanone
Canonical SMILESOC1=CC=C(/C=C2OC(C)=CC\2=O)C=C1O
分子式C12H10O4
分子量218.2
溶解度≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 0.03 and 0.36 μM for COX-2 and COX-1, respectively

Inotilone is a cyclooxygenase (COX) inhibitor.

Many of nonsteroidal anti-inflammatory drugs (NSAIDs) target cyclooxygenases (COX), which catalyze the first two steps in the biosynthesis of the prostaglandins from the substrate arachidonic acid.

In vitro: Inotilone was tested as the inhibitor of mitogen-activated protein kinase, nuclear factor-κB (NF-κB), and matrix-metalloproteinase (MMP)-9 protein expressions in LPS-stimulated RAW264.7 cells. When RAW264.7 macrophages were treated with inotilone with LPS, a significant concentration-dependent inhibition of NO production was detected. It was also found that inotilone could block the protein expression of iNOS, NF-κB, and MMP-9 in LPS-stimulated RAW264.7 macrophages [1].

In vivo: In in vivo tests, inotilone decreased the paw edema after Carr administration, and it increased the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx). Inotilone also significantly attenuated the malondialdehyde (MDA) level in the edema paw. Inotilone decreased the NO and tumor necrosis factor (TNF-α) levels on serum after Carr injection. In addition, an intraperitoneal injection treatment with inotilone could diminish neutrophil infiltration into sites of inflammation, as did indomethacin [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Huang GJ, Huang SS, Deng JS.  Anti-inflammatory activities of inotilone from Phellinus linteus through the inhibition of MMP-9, NF-κB, and MAPK activation in vitro and in vivo. PLoS One. 2012;7(5):e35922.