trans-AUCB_可溶性环氧化物水解酶(sEH)的有效抑制剂_885012-33-9_Apexbio

DAPT markedly increased t-AUCB-induced apoptosis of U251 and U87 cells. Moreover, T-AUCB alone did not obviously affect caspase-3 activity in the cells, but t-AUCB plus DAPT pretreatment caused significant increase of caspase-3 activity. In addition, the pretreatment with DAPT was able to completely block t-AUCB-induced phosphorylation of p38 MAPK, MAPKAPK2 and Hsp27 in the cells [1]. In vivo: A previous animal study was conducted to investigate the effects of acute sEH inhibition by t-AUCB on infarct volume, functional outcome, and changes in cerebral blood flow (CBF) in a rat model of ischemic stroke. It was found that t-AUCB could significantly reduce cortical infarct volume by 35%, elevate cumulative epoxyeicosatrienoic acids-to-dihydroxyeicosatrienoic acids ratio in brain cortex by twofold, and improve functional outcome in arm-flexion test when compared with that of the vehicle-treated group [2]. Clinical trial: So far, no clinical study has been conducted. 参考文献:
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IC50: 0.5 nM trans-AUCB is a potent inhibitor of soluble epoxide hydrolase (sEH). Soluble epoxide hydrolase (sEH) can convert epoxides to their corresponding diols. Inhibitors of sEH have anti-hypertensive, anti-inflammatory, neuroprotective, and cardioprotective effects. In vitro: A previous study showed that the pretreatment with DAPT could substantially potentiate the growth inhibition caused by t-AUCB in U251 and U87 cells. Moreover, the pretreatment with
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化学性质
产品名: trans-AUCB 修订日期: 6/30/2016
产品名: Cas No.: 分子量: 分子式: 化学名:
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源自文库
trans-AUCB
885012-33-9 412.5
//struct//
C24H32N2O4
4-[[trans-4-[[(tricyclo[3.3.1.13,7]dec-1-ylamino)carbonyl]amino]cycl ohexyl]oxy]-benzoic acid
O=C(O)C(C=C1)=CC=C1O[C@H]2CC[C@H](NC(N[C@@]34CC5C[C@H ](C[C@H](C5)C4)C3)=O)CC2
Soluble in DMSO
Store at -20°C
For obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.
Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
生物活性
靶点 :
Metabolism
信号通路:
Hydrolase
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