ML077-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

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ML077

Cat.No.:HY-115606

CASNo.:1135304-61-8

分⼦式:C₁₇H₁₆N₄OS₂

分⼦量:356.47

作⽤靶点:NKCC;EndogenousMetabolite

作⽤通路:MembraneTransporter/IonChannel;Metabolic

Enzyme/Protease

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性ML007是⼀种针对神经元特异性钾-氯协同转运蛋⽩2(KCC2)的选择性拮抗剂，其对于KKC2的IC50为537

nM，⽽对KKC1的抑制活性极弱(IC5050μM)。ML077通过抑制KCC2的氯离⼦外排功能，提⾼细胞内氯

离⼦浓度，从⽽增强氯离⼦通道介导的去极化作⽤。ML007可不依赖KATP通道促进葡萄糖刺激的胰岛素分泌

(GSIS)。ML007可⽤于研究疼痛、癫痫和胰岛素分泌等⽅⾯的功能。

REFERENCES

[1].DelpireE,etal.FurtheroptimizationoftheK-ClcotransporterKCC2antagonistML077:developmentofahighlyselectiveandmore

potentinvitroprobe.BioorgMedChemLett.2012Jul15;22(14):4532-5.

[2].KursanS,McMillenTS,BeesettyP,Dias-JuniorE,AlmutairiMM,SajibAA,KozakJA,Aguilar-BryanL,DiFulvioM.TheneuronalK+Cl-

co-transporter2(Slc12a5)modulatesinsulinsecretion.SciRep.2017May11;7(1):1732.doi:10.1038/s41598-017-01814-0.PMID:

PMCID:PMC5431760.

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