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Inhibitors?ScreeningLibraries?Proteins

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Darapladib(Standard)

Cat.No.:HY-10521R

CASNo.:356057-34-6

Synonyms:SB-480848(Standard)

分?式:C??H??F?N?O?S

分?量:666.77

作?靶点:Phospholipase;Apoptosis

作?通路:MetabolicEnzyme/Protease;Apoptosis

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Darapladib(Standard)是Darapladib的分析标准品。本产品?于研究及分析应?。Darapladib(SB-480848)

是?种具有?服活性、选择性且可逆的Lp-PLA2抑制剂(IC50=0.25nM)。Darapladib可触发对神经胶质瘤细

胞凋亡的不可逆作?并诱导周期停滞。Darapladib可?于动脉粥样硬化和癌症的研究。

IC50TargetIC50:0.25nM(Lp-PLA2)[1]

REFERENCES

[1].BlackieJA,etal.TheidentificationofclinicalcandidateSB-480848:apotentinhibitoroflipoprotein-associatedphospholipaseA2.Bioorg

MedChemLett.2003Mar24;13(6):1067-70.

[2].HuMM,etal.Theinhibitionoflipoprotein-associatedphospholipaseA2exertsbeneficialeffectsagainstatherosclerosisinLDLR-

deficientmice.ActaPharmacolSin.2011Oct;32(10):1253-1258.

[3].WangYJ,etal.Theselectivelipoprotein-associatedphospholipaseA2inhibitord