LEI-401-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemELEI-401Cat.No.:HY-131181CASNo.:2393840-15-6分⼦式:C₂₄H₃₁N₅O₂分⼦量:421.54作⽤靶点:Phospholipase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(237.23mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3723mL11.8613mL23.7225mL5mM0.4745mL2.3723mL4.7445mL10mM0.2372mL1.1861mL2.3723mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.93mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LEI-401⼀种⾸创的、选择性的、通过⾎脑屏障的NAPE-PLD(N-酰磷酰⼄醇胺磷脂酶D)抑制剂，IC50为1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE27nM。LEI-401对⼩⿏情绪⾏为的调节。体外研究LEI-401reducedabroadrangeofNAEsincludinganandamideinneuronalcellsinaNAPE-PLD-dependentmanner.LEI-401(0.04-20μM;30ꢀminutes)dose-dependentlyreducesthelabelingofNAPE-PLDwithanIC50of0.86μMinhNAPE-PLD-transfectedHEK293Tcells.LEI-401reducesNAElevelsinNeuro-2acells,butnotinNAPE-PLDKOcells[1].体内研究LEI-401(30ꢀmg/kg;i.p.)diminishesfearextinctioninmice[1].LEI-401alsoactivatesHPAaxissignaling[1].LEI-401(10mg/kg;p.o.)treatmentshowsthet1/2,Cmax,tmax,AUClast,andFvaluesof2.5hours,1370ng/mL,2hours,6760h*ng/mL,and25%,respectively[1].LEI-401(30mg/kg;i.p.)treatmentshowtheCmax,tmax,AUClast,andFvaluesof10300ng/mL,1hour,38600h*ng/mL,and48%,respectively[1].AnimalModel:Male7–12-week-oldC57BL/6Jmice[1]Dosage:30ꢀmg/kgAdministration:I.p.Result:Producedasignificantincreaseinfreezingascomparedtovehicle.AnimalModel:C57BL/6Jmice[1]Dosage:10mg/kgAdministration:P.o.(PharmacokineticAnalysis)Result:Thet1/2,Cmax,tmax,AUClast,andFvalueswere2.5hours,1370ng/mL,2hours,6760h*ng/mL,and25%,respectively.REFERENCES[1].MockED,etal.DiscoveryofaNAPE-PLDinhibitorthatmodulatesemotionalbehaviorinmice.NatChemBiol.2020;16(6):667-675.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus