MAO-A-5-HT2AR-IN-1-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMAO-A/5-HT2AR-IN-1Cat.No.:HY-151596CASNo.:2769156-00-3分⼦式:C₃₀H₂₈FN₃O₂分⼦量:481.56作⽤靶点:MonoamineOxidase;5-HTReceptor作⽤通路:NeuronalSignaling;GPCR/GProtein储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性MAO-A/5-HT2AR-IN-1(compoundI14)⼀种有效的MAO-A和5-HT2AR双重抑制剂，其IC50分别为0.004和0.014μM。MAO-A/5-HT2AR-IN-1⼀种潜在的抗抑郁剂。IC50&TargetMAO-A5-HT2AReceptorMAO-B0.004±0.μM(IC50)0.014μM(IC50)1.05±0.0μM(IC50)体外研究MAO-A/5-HT2AR-IN-1(compoundI14)(0-4μM,24h)exhibitsasignificantneurocytoprotectiveeffectontheCORT-inducedcelldepressionmodel[1].MAO-A/5-HT2AR-IN-1isabletooccupytheactivecavityof5-HT2ARandMAO-Awithmultiplehydrogenbondingforcesandπ–πstackinginteraction[1].MAO-A/5-HT2AR-IN-1exhibitslowproliferationinhibitoryactivitiesagainstL02cells(IC50>100μM),SH-SY5Y(IC50>10μM)andPC12(IC50>10μM),indicatingithasagoodsafetyprofile[1].[1][1]CellLine:PC12cellsConcentration:4.0,2.0,1.0,and0.5μM(and500μMCORT)IncubationTime:24hResult:ShowedasignificantprotectiveeffectonPC12cellsinjuryatdifferentconcentrationscomparedwiththemodelgroup,wherethebestprotectiveeffectwasobservedat0.5μM.1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究MAO-A/5-HT2AR-IN-1(compoundI14)(10and20mg/kg)significantlyamelioratesthedepression-likebehaviorofmice[1].MAO-A/5-HT2AR-IN-1(0-1μM,for7days)improveszebrafishlocomotionandthedepression-likebehavior[1].MAO-A/5-HT2AR-IN-1isabletorepairthedamageofmicehippocampalneuronalcellsandreducetheexpressionof5-HT2ARinmicebraintissue[1].MAO-A/5-HT2AR-IN-1(2mg/kg(i.v.)10mg/kg(i.g.);once)hasagoodclearancerateof345.69mL/min/kginrats[1].AnimalModel:ICRmalemice(8−10weeksold,weight18-20g)[1]Dosage:10mg/kg,20mg/kgAdministration:For2weeksResult:Significantlyimproveddepression-likebehaviorinmice,withthelowdosegroup(10mg/kg)beingmorepotentthanwiththepositivedrug(Flu,20mg/kg).Hadnorelevanttoxiceffectsontheliver,kidney,lung,andspleenofmiceduringthetreatmentperiod.AnimalModel:Zebrafish(ABstrain,Reserpine-inducedzebrafishdepressionmodel)[1]Dosage:0.1,0.5,1μMCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Administration:Given24hafterreserpine,for7days.Tel:400-820-3792ax-mail:tech@MedChemEResult:ShowedthatzebrafishintheI14administeredgroupmovedsignificantlymoredistance,faster,andspentsignificantlymoretimeintheupperpartcomparedtothemodelgroup.AnimalModel:Sprague-Dawleyrats(male)[1]Dosage:2mg/kg(i.v.)10mg/kg(i.g.)Administration:IV,IG;once(PharmacokineticAnalysis)Result:PharmacokineticParametersofMAO-A/5-HT2AR-IN-1inmaleSprague-Dawleyrats[1].parameter2mg/kg(i.v.)10mg/kg(i.g.)Tmax(h)0.08±0.001.33±0.33Cmax(ng/mL)673.33±25.4199.67±6.01AUC0-24(ng/mL∗h)2230.67±153.78490.67±70.43AUC0-inf(ng/mL∗h)2322.67±178.02504.00±71.08t1/2(h)6.31±0.555.22±0.79CL

(mL/min/kg)14.54±1.20345.69±53.40MRTinf(h)4.19±0.144.94±0.36F(%)4.40REFERENCES[1].SunX,LiN,etal.Developmen