Elcubragistat-ABX-1431-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEElcubragistatCat.No.:HY-117632CASNo.:1446817-84-0Synonyms:ABX-1431分?式:C??H??F?N?O?分?量:507.39作?靶點(diǎn):MAGL作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(246.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9709mL9.8544mL19.7087mL5mM0.3942mL1.9709mL3.9417mL10mM0.1971mL0.9854mL1.9709mL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(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.10mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.10mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.10mM);ClearsolutionBIOLOGICALACTIVITY?物活性Elcubragistat(ABX-1431)?種?效，選擇性和?服可?的CNS-滲透性單酰?油脂酶(MAGL)抑制劑，IC50為14nM。IC50&TargetIC50:14nM(humanMGLL)[1]體外研究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].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatCommun.2022Feb25;13(1):1058.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].CisarJS,etal.IdentificationofABX-1431,aSelectiveInhibitorofMonoacylglycerolLipaseandClinicalCandidateforTreatmentofNeurologicalDisorders.JMedChem.2018Oct25;61(20):9062-9084.McePdfHeightCaution:Producthasnotbeen