CypD-IN-7-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

CypD-IN-7

Cat.No.:HY-179417

分⼦式:C₄₁H₄₄ClFN₆O₅

分⼦量:755.28

作⽤靶点:Cyclophilin

作⽤通路:Immunology/Inflammation

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性CypD-IN-7是⼀种强效的CyclophilinD(CypD/PPIF)抑制剂,可抑制CypD的PPIase活性(Ki=2.4nM),具有

线粒体通透性转换孔(MPTP)开放保护作⽤。CypD-IN-7可⽤于胰腺炎研究[1]。

IC50TargetCyclophilinD

2.4nM(Ki)

体外研究CypD-IN-7(18f)(39nM-5μM)increasesmitochondrialcalciumretentioncapacity(CRC)inisolatedmouse

livermitochondria[1].

CypD-IN-7(10μM)markedlyincreasesmitochondrialcalciumretentioncapacity(CRC),andprovides

significantlysuperiorprotectionagainstMPTPopeningversuscyclosporinA(CsA)at300nM[1].

体内研究CypD-IN-7(18f)(50mg/kg;i.p.;dosedimmediatelyafterthe3rdand6thCaerulein(HY-A0190)injections

and2hafterthe7thinjection)significantlyreducesserumamylase,pancreaticMPOactivity,

edema/inflammationscores,andtotalhistologyscoreinacaerulein-inducedacutepancreatitis(CER-AP)

mousemodel,whereas20mg/kgshowsnosignificanteffect[1].

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