PDE1-IN-7--生命科学试剂-MCE.pdf

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PDE1-IN-7

Cat.No.:HY-161506

CASNo.:3027833-49-1

分⼦式:C₃₂H₃₆F₂N₂O₆S

分⼦量:614.7

作⽤靶点:Phosphodiesterase(PDE)

作⽤通路:MetabolicEnzyme/Protease

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性PDE1-IN-7(Compound13h)是bPDE1的选择性抑制剂(IC50=10nM)。在BDL诱导的肝纤维化⼤⿏模型中表

现出显著的抗纤维化效果。PDE1-IN-7可以⽤于肝纤维化⽅⾯的研究[1]。

IC50TargetPDEI

10nM(IC50)

体外研究PDE1-IN-7(2.5-20μM;48h)effectivelyinhibitsTGF-β-inducedmyofibroblastdifferentiationandproliferation

inLX-2cells[1].

WesternBlotAnalysis[1]

CellLine:humanstellatecellLX-2

Concentration:2.5,5,10,20μM

IncubationTime:48h

Result:Dose-dependentlyreducedtheelevatedexpressionlevelsoffibronectin,collagenI,and

α-SMAinducedbyTGF-βinLX-2cells.

体内研究PDE1-IN-7(i.p.;2.5mg/kg;oncedailyfor21days)showssignificantantifibroticeffectsinaratmodelofbile

ductligation-inducedhepaticfibrosis[1].