5-HT6R-FAAH-modulator-1-生命科学试剂-MCE.pdfVIP

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5-HT6R/FAAHmodulator1

Cat.No.:HY-175816

分⼦式:C₂₆H₃₄N₆O₄

分⼦量:494.59

作⽤靶点:5-HTReceptor;FAAH;Apoptosis;ReactiveOxygenSpecies

(ROS)

作⽤通路:GPCR/GProtein;NeuronalSignaling;Metabolic

Enzyme/Protease;Apoptosis;Immunology/Inflammation;NF-κ

B

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性5-HT6R/FAAHmodulator1是⼀种选择性⾎清素5-HT6受体配体和脂肪酸酰胺⽔解酶(FAAH)抑制剂。5-

HT6R/FAAHmodulator1对5-HT6的pKi为6.33，对FAAH的pIC50为6.33。5-HT6R/FAAHmodulator1对

⼄酰胆碱酯酶(AChE)或丁酰胆碱酯酶(BChE)(pIC50=5.12)也有轻微抑制作⽤。5-HT6R/FAAHmodulator1

能够抑制细胞凋亡(apoptosis)并降低活性氧(ROS)⽔平。5-HT6R/FAAHmodulator1可⽤于神经系统疾病的

研究，如阿尔茨海默病(AD)[1]。

IC50Target5-HT6Receptor

6.33(pKi)

体外研究5-HT6R/FAAHmodulator1(Compound23)(0.3-30μM,72h)inhibitsHepG2andSH-SY5Ycellsgrowth[1].

5-HT6R/FAAHmodulator1(10μM,17h)increasescellviabilityandinhibitsapoptosisandreducesROS

levelsinAβ1-42-treatedHT-22cells[1].

5-HT6R/FAAHmodulator1(0.03-0.15μM)showspotentantioxidantactivity[1].

CellViabilityAssay[1]