trans-AUCB |
| Catalog No.GC12755 |
trans-AUCB (t-AUCB) es un inhibidor de epÓxido hidrolasa (sEH) soluble potente, activo por vÍa oral y selectivo con IC50 de 1,3 nM, 8 nM, 8 nM para hsEH, sEH de ratÓn y sEH de rata, respectivamente. trans-AUCB tiene actividad anti-glioma.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 885012-33-9
Sample solution is provided at 25 µL, 10mM.
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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 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.
References:
[1] Li JY, Li RJ, Wang HD. γ-secretase inhibitor DAPT sensitizes t-AUCB-induced apoptosis of human glioblastoma cells in vitro via blocking the p38 MAPK/MAPKAPK2/Hsp27 pathway. Acta Pharmacol Sin. 2014 Jun;35(6):825-31.
[2] Shaik JS, Ahmad M, Li W, Rose ME, Foley LM, Hitchens TK, Graham SH, Hwang SH, Hammock BD, Poloyac SM. Soluble epoxide hydrolase inhibitor trans-4-[4-(3-adamantan-1-yl-ureido)-cyclohexyloxy]-benzoic acid is neuroprotective in rat model of ischemic stroke. Am J Physiol Heart Circ Physiol. 2013 Dec 1;305(11):H1605-13.
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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