JZL195-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJZL195Cat.No.:HY-15250CASNo.:1210004-12-8分⼦式:C₂₄H₂₃N₃O₅分⼦量:433.46作⽤靶点:FAAH;MAGL;Autophagy作⽤通路:MetabolicEnzyme/Protease;NeuronalSignaling;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(115.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3070mL11.5351mL23.0702mL5mM0.4614mL2.3070mL4.6140mL10mM0.2307mL1.1535mL2.3070mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.77mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.77mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JZL195⼀种有效选择的脂酸酰胺⽔解酶(FAAH)和单酰⽢油脂酶(MAGL)双重抑制剂，IC50s分别为2和4nM[1]。IC50&TargetIC50:2nM(FAAH),4nM(MAGL)[1]体外研究JZL195producesnear-completeblockadeofFP-RhlabelingofbothmousebrainFAAHandMAGLatconcentrationsaslowas100nM(IC50valuesof13and19nM,respectively)[1].JZL195inhibitsratandhumanFAAHandMAGLenzymeswithIC50valuesintherangeof≈10-100nMbasedoncompetitiveABPPassays[1].体内研究JZL195(20mg/kg;i.p.)producesanantinociceptiveresponseinthetailimmersionassay[1].AnimalModel:MaleC57BL/6Jmice[1]Dosage:20mg/kgAdministration:IntraperitonealinjectionResult:ProducedamuchgreaterantinociceptiveresponseinthetailimmersionassaycomparedwithinhibitorsofeitherFAAHorMAGLalone.户使⽤本产品发表的科研⽂献•CellDeathDiffer.2022Sep14.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LongJZ,etal.DualblockadeofFAAHandMAGLidentifiesbehavioralprocessesregulatedbyendocannabinoidcrosstalkinvivo.ProcNatlAcadSciUSA.2009Dec1;106(48):20270-5.[2].AndersonWB,etal.ActionsofthedualFAAH/MAGLinhibitorJZL195inamurineinflammatorypainmodel.Neuropharmacology.2014Jun;81:224-30.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc