Elcubragistat-ABX-1431-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEElcubragistatCat.No.:HY-117632CASNo.:1446817-84-0Synonyms:ABX-1431分⼦式:C₂₀H₂₂F₉N₃O₂分⼦量:507.39作⽤靶点:MAGL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:125mg/mL(246.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9709mL9.8544mL19.7087mL5mM0.3942mL1.9709mL3.9417mL10mM0.1971mL0.9854mL1.9709mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.10mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.10mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.10mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Elcubragistat(ABX-1431)⼀种⾼效，选择性和⼝服可⽤的CNS-渗透性单酰⽢油脂酶(MAGL)抑制剂，IC50为14nM。IC50&TargetIC50:14nM(humanMGLL)[1]体外研究Elcubragistat(ABX-1431)isapotenthumanMGLLinhibitor(IC50=0.014µM)with>100-foldselectivityagainstABHD6and>200-foldselectivityagainstPLA2G7.ElcubragistatinhibitshumanPC3cellswithanIC50of0.0022µM.Inthecell-basedassay,>100-foldselectivityforMGLLoverABHD6(IC50=0.253µM)andPLA2G7(IC50=494µM)ismaintained[1].体内研究Elcubragistat(ABX-1431)inhibitsMGLLactivityinrodentbrain(ED50=0.5-1.4mg/kg),increasesbrain2-AGconcentrations,andsuppressespainbehaviorintheratformalinpainmodel[1].PROTOCOLCellAssay[1]HumanprostatecancerPC3cellsaregrowninF-12Kmediumsupplementedwith10%fetalbovineserumat37°Cwith5%CO2to80%confluencyin100mmdishes.ABX-1431isaddedtocellstogivefinalconcentrationof0.1-10µMcompoundinserumfreemedia.Cellsareincubatedfor30min.Cellsarewashed,harvested,andlysedbyprobesonication.Celllysates(2mg/mL)aretreatedwithJW912(1µM)andanalyzedbySDSandin-gelfluorescencescanning[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats[1]Administration[1]Elcubragistatisadministeredinavolumeof5mL/kg.MaleICRmiceormaleSpragueDawleyrats6to12weeksareadministeredsingleoraldosesofElcubragistat(0.5-32mg/kgformiceand0.03-10mg/kgforrats).FourhoursafterElcubragistatadministration,animalsareanesthetized.Followingbloodcollection,animalsarekilledbydecapitationandbrainsareremoved,hemisectedandfrozeninliquidnitrogenforanalysis[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2022Feb25;13(1):1058.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].CisarJS,etal.IdentificationofABX-1431,aSelectiveInhibitorofMonoacylglycerolLipaseandClinicalCandidateforTreatmentofNeurologicalDisorders.JMedChem.2018Oct25;61(20):9062-9084.McePdfHeightCaution:Producthasnotbeen