VU0448088-ML253-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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VU0448088

Cat.No.:HY-162663

CASNo.:1417616-42-2

Synonyms:ML253

分⼦式:C₁₆H₁₅ClN₄OS

分⼦量:346.83

作⽤靶点:mAChR

作⽤通路:GPCR/GProtein;NeuronalSignaling

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性VU0448088(ML253)是⼀种有效的、可穿过⾎脑屏障的三环毒蕈碱⼄酰胆碱受体亚型4(tricyclicmuscarinic

acetylcholinereceptorsubtype4(M4))正变构调节剂，对⼈和⼤⿏的EC50值分别为56,176nM。

VU0448088具有⽤于精神病研究的潜⼒[1][2]。

IC50TargetmAChR4

56nM(EC50)

体内研究VU0448088(3,10,30,56.6,100mg/kg;i.p.)reversesamphetamine-inducedhyperlocomotioninadose-

dependentmanner[1].

AnimalModel:Rat(amphetamine-inducedhyperlocomotion)[1]

Dosage:3,10,30,56.6,100mg/kg

Administration:IP

Result:Reversedamphetamine-inducedhyperlocomotioninadose-dependentmanner,showed

amodestreductionof26%atadoseof10mg/kg;atthethreehighestdoses(30,56.6

and100mg/kg),showedsignificantreductionsof47.9%,53.7%and57.3%,respectively.

REFERENCES

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