MSI-1436-lactate-Trodusquemine-lactate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMSI-1436lactateCat.No.:HY-12219ACASNo.:1309370-86-2Synonyms:Trodusqueminelactate;Aminosterol-1436lactate分⼦式:C₃₇H₇₂N₄O₅S.₇/₂C₃H₆O₃分⼦量:1000.17作⽤靶点:Phosphatase作⽤通路:MetabolicEnzyme/Protease储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:54mg/mL(53.99mM;Needultrasonicandwarming)0.1MHCL:50mg/mL(49.99mM;ultrasonicandadjustpHto4withHCl)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9998mL4.9992mL9.9983mL5mM0.2000mL0.9998mL1.9997mL10mM0.1000mL0.4999mL0.9998mL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(sealedstorage,awayfrommoisture)。-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：5%DMSO>>40%PEG300>>5%Tween-80>>50%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥3mg/mL(3.00mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性MSI-1436lactate具有选择性的PTP1B的⾮竞争性抑制剂，其IC50值为1μM，⽽对TCPTP的IC50值为224μM。IC50&TargetIC50:1μM(PTB1B),224μM(TCPTP)[1]体外研究MSI-1436'sinhibitionofTCPTPisapproximatelytwologslessthantheeffectonPTP1Bactivity,witharesultingIC50valueof224µM[1].MSI-1436(Trodusquemine,10μM)restoresERKphosphorylationinresponsetomGluR1/5agonistDHPGinF11neuronalcells.MSI-1436(10uM)rescuesDHPG-inducedholdingcurrentsandrestoresDSIinLMO4KOBLAneurons[2].MSI-1436(0.1-100µM)blocksPTP1Bactivity[3].体内研究MSI-1436(10mg/kg,i.p.)causesobesity-dependentbodyweight,reducestotalbodyfatcontentandadipocytesizeandlipidcontentofwhiteadiposetissueofmice[1].MSI-1436(Trodusquemine)exhibitsanxiolyticeffectthrougharestorationofendocannabinoid(eCB)signalingwithintheamygdala[2].MSI-1436(5mg/kg,i.p.)hasananti-diabeticeffectondiabeticmice,andissufficienttosuppressfoodintakeandcauseweightlossinCD1mice[3].PROTOCOLCellAssay[1]Quantitationofphosphataseactivityismeasuredusinganintactcellassay.HepG2cellsarepretreatedwith10μMMSI-1436lactateorsodiumorthovanadate(100μM,postivecontrol)for10minat37°C,thenincubatedwith10μMpNPP(acellpermeablehydrolysablesubstrate)for30minat37°C.SamplesofthesupernatantsarespectrophotometricallyanalyzedatOD405forhydolyzedpNP,adirectendproductofphosphataseactivity[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMaleAKR/Jmicearerandomlyplacedonadlibitum10,45,or60%fatkcaldiets.After14weeks,miceareAdministration[1]randomlyassignedtothreetreatmentgroups(n=5to8mice/group);MSI-1436lactate(initialdoseof10mg/kgwiththreesubsequentweeklydosesof5mg/kg,intraperitoneally),vehicle(saline,10mL/kg,weekly4×),orpair-fed(PF).PFanimalsareinjectedwithsaline(weekly4×)andallottedtheamountoffoodconsumeddailybyMSI-1436lactate-treatedanimals.Onday23,miceareanesthetizedandeuthanizedforbloodandtissuecollection,respectively.Plasmaisobtainedfollowingcentrifugationofblood14,000rpmfor10minat4°C[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CommunBiol.2021Feb24;4(1):248.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].LantzKA,etal.InhibitionofPTP1Bbytrodusquemine(MSI-1436)causesfat-specificweightlossindiet-inducedobesemice.Obesity(SilverSpring).2010Aug;18(8):1516-1523.[2].QinZ,etal.Chronicstressinducesanxietyviaanamygdalarintracellularcascadethatimpairsendocannabinoidsignaling.Neuron.2015Mar18;85(6):1319-31.[3].QinZ,etal.FunctionalpropertiesofClaramine:anovelPTP1Binhibitorandmimeticcompound.BiochemBiophysResCommun.2015Feb27;458(1):21-7