MT-228-BPN-0026709-生命科学试剂-MCE.pdfVIP

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MT-228

Cat.No.:HY-175199

CASNo.:2404652-24-8

Synonyms:BPN-0026709

分⼦式:C₁₉H₁₉N₃O₃

分⼦量:337.37

作⽤靶点:Myosin

作⽤通路:Cytoskeleton

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性MT-228是⼀种选择性且具有⾎脑屏障通透性的⾮肌⾁肌球蛋⽩II(non-musclemyosinII)抑制剂。MT-228通

过选择性靶向⾮肌⾁肌球蛋⽩II(non-musclemyosinII)(KI=1.5μM)⽽⾮⼼脏肌球蛋⽩II(CMII)(KI=17μ

M)显著改善了耐受性，并且SmMllMD的序列与NMllB的序列有83.6%的⼀致性。MT-228在精神活性物质

使⽤障碍的动物模型中显⽰出持久的效果[1]。

体外研究MT-228(10-3-100μM)showsimprovedcardiacsafetyandselectivitycomparedtoBlebbistatin(HY-13813)

withaKINMIIBof1.5μMinanATPaseassay[1].MT-228showsexcellentagreementwiththecytokinesis

(EC50=1.0μM)[1].

体内研究MT228(5-10mg/kg,i.p.,singledose)iswell-tolerateduptoatleast10mg/kginmice[1].MT-228(0.5-5

mg/kg,i.p.ori.v.,singledose)disruptsthemotivationforstimulantinmiceandrats[1].

AnimalModel:8-10-week-oldmaleC57BL/6mice(25-30g)[1]

Dosage:i.p.forasingledose

Administration:5,7.5,10mg/kg

Result:Showed