Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemELEI-401Cat.No.:HY-131181CASNo.:2393840-15-6分?式:C??H??N?O?分?量:421.54作?靶點(diǎn):Phospholipase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(237.23mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3723mL11.8613mL23.7225mL5mM0.4745mL2.3723mL4.7445mL10mM0.2372mL1.1861mL2.3723mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.93mM);ClearsolutionBIOLOGICALACTIVITY?物活性LEI-401?種?創(chuàng)的、選擇性的、通過?腦屏障的NAPE-PLD(N-酰磷酰?醇胺磷脂酶D)抑制劑，IC50為1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE27nM。LEI-401對??情緒?為的調(diào)節(jié)。體外研究LEI-401reducedabroadrangeofNAEsincludinganandamideinneuronalcellsinaNAPE-PLD-dependentmanner.LEI-401(0.04-20μM;30?minutes)dose-dependentlyreducesthelabelingofNAPE-PLDwithanIC50of0.86μMinhNAPE-PLD-transfectedHEK293Tcells.LEI-401reducesNAElevelsinNeuro-2acells,butnotinNAPE-PLDKOcells[1].體內(nèi)研究LEI-401(30?mg/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:30?mg/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