FABP4-5-IN-6-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

FABP4/5-IN-6

Cat.No.:HY-178471

CASNo.:2975215-64-4

分⼦式:C₂₁H₁₆Cl₂FNO₃

分⼦量:420.26

作⽤靶点:FABP;InterleukinRelated

作⽤通路:MetabolicEnzyme/Protease;Immunology/Inflammation

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性FABP4/5-IN-6是⼀种⼝服有效的强效FABP4/5抑制剂(Ki=0.41/2.53μM),对FABP3的选择性较低(Ki=

59.72μM)。FABP4/5-IN-6可抑制Lipopolysaccharides(HY-D1056)(LPS)诱导的THP-1巨噬细胞中MCP-1

和IL-6的分泌。FABP4/5-IN-6具有显著的抗炎作⽤,并能减轻LPS诱导的肝损伤。FABP4/5-IN-6对hERG通

道的抑制作⽤较弱(LD502000mg/kg)。FABP4/5-IN-6可⽤于炎症相关疾病的研究[1]。

体外研究FABP4/5-IN-6(CompoundY18)(80μM,24h)showsnosignificantcytotoxicitytoTHP-1cells,andcell

viabilityisunaffected[1].

FABP4/5-IN-6(5-25μM,24h)significantlyinhibitsLPS-inducedsecretionofMCP-1andIL-6inTHP-1

macrophagecells,withtheinhibitoryeffectshowingadose-dependenteffect[1].

ELISAAssay[1]

CellLine:LPS-inducedTHP-1macrophagecells

Concentration:5μM,10μM,25μM

IncubationTime:Incubate18hours,thenstimulatewithLPS(100ng/mL)for6hours

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