M3-mAChR-agonist-1-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

M3mAChRagonist1

Cat.No.:HY-131196

CASNo.:1624297-26-2

分⼦式:C₂₉H₃₃F₃N₆O₄S

分⼦量:618.67

作⽤靶点:mAChR

作⽤通路:GPCR/GProtein;NeuronalSignaling

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性M3mAChRagonist1是⼀种优先作⽤于M3亚型的M3/M5mAChR双重正向变构调节剂(PAM)。M3mAChR

agonist1对包括M1、M2和M4mAChR在内的其他mAChR亚型具有优异的亚型选择性。M3mAChR

agonist1通过调节M3毒蕈碱⼄酰胆碱受体,增加离体⼤⿏膀胱条的收缩,从⽽增强信号通路。

IC50TargetmAChR3mAChR5

体外研究M3mAChRagonist1(compound9;1-10µM)enhancestheactionofACh,whichisreleasedfromnerves

throughelectricalfieldstimulation(EFS),resultinginincreasingcontractionofisolatedratbladderstrips[1].

REFERENCES

[1].TanakaH,etal.Discoveryandstructure-activityrelationshipsstudyofpositiveallostericmodulatorsoftheM3muscarinicacetylcholine

receptor.BioorgMedChem.2020Jul1;28(13):115531.

McePdfHeight

Caution:Producthasnotbeenfullyvalidatedformedicalapplicati

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