sEH-FLAP-IN-2-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

sEH/FLAP-IN-2

Cat.No.:HY-179441

分⼦式:C₂₆H₃₃N₅O₂

分⼦量:447.57

作⽤靶点:EpoxideHydrolase;FLAP

作⽤通路:MetabolicEnzyme/Protease;Immunology/Inflammation

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性sEH/FLAP-IN-2是⼀种选择性sEH(IC50=12.6nM)/FLAP双重抑制剂。sEH/FLAP-IN-2可显著减少5-

LOX/FLAP和sEH衍⽣的脂质体,从⽽促进脂质体的重新分布。sEH/FLAP-IN-2可⽤于腹膜炎的研究[1]。

体外研究sEH/FLAP-IN-2(Compound6)showsnosignificantinhibitoryactivityagainst5-LOX,withanIC50value10

μM[1].

sEH/FLAP-IN-2(10μM,15min)significantlyinhibitstheformationof5-LOXproducts(LTB4,trans-LTB4,and

5-HETE)intheFLAP-dependentsystemwithoutexogenousarachidonicacid(AA)inhumanneutrophils,with

aresidualactivityof35.7%;inthepresenceofexogenousAA,itsinhibitoryactivitywasweakened(IC5010

μM)[1].

sEH/FLAP-IN-2(0.1-10μM,16min)hasnosignificanteffectontheactivitiesofCOX-1,COX-2,andmPGES-

1[1].

sEH/FLAP-IN-2(0.1-10μM,120min)concentration-dependentlyinhibits5-LOX/FLAP-derivedmediators

(suchasLTB4andLTC4),es

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