DMP-777-L-694458-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDMP777Cat.No.:HY-75957CASNo.:157341-41-8Synonyms:L-694458分⼦式:C₃₁H₄₀N₄O₆分⼦量:564.67作⽤靶点:Elastase作⽤通路:MetabolicEnzyme/Protease储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:38.33mg/mL(67.88mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7709mL8.8547mL17.7095mL5mM0.3542mL1.7709mL3.5419mL10mM0.1771mL0.8855mL1.7709mL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(storedundernitrogen)。-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(4.43mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.43mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.43mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.43mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DMP777⼀种有效的，选择性的，可⼝服的humanleukocyteelastase(HLE)抑制剂。IC50&TargetHumanleukocyteelastase(HLE)[2]体内研究DMP-777-treatedratsshowamarkeddecreaseinH/K-ATPasestainingparietalcells.DMP-777-inducedlossofparietalcellsissignificantlyamelioratedwithcoadministrationofomeprazole.DMP-777-treatedanimalsdemonstratesmarkedfoveolarhyperplasiainthefunduswithprominentexpansionofdiastase-resistant,PAS-positivesurfacemucouscells.WhenDMP-777iscoadministeredwithomprazole,thereisasignificantdecreaseinBrdUpositiveS-phasecellscomparedwithratsthatreceiveDMP-777alone[1].Afteroraldosingofmonkeysat40mg/kgwithDMP-777theonlystereoisomerdetectedinthepost-doseplasmasamplesisthestartingmaterialDMP-777,andnoinversionoftheconfigurationatpositions'a'and'b'ofDMP-777hasoccurredinvivo[2].Mist1-/-micetreatedwithDMP-777showfewerchiefcelltoSPEMtransitions.Mist1-/-micetreatedwithL635demonstratessignificantlyfewerproliferativeSPEMcellscomparedtocontrolmice[3].PROTOCOLAnimalGroups1Aand1BreceivecontrolvehicleinsteadofomeprazoleandDMP-777.Group2Aand2BaredosedAdministration[1]withDMP-777oncedailyonStudyDay3orDays3and4,respectively,andreceivecontrolvehicleinsteadofomeprazole.Groups3Aand3BaretreatedwithomeprazoletwicedailyonStudyDays1to3orDays1to4,respectively,andreceivecontrolvehicleinsteadofDMP-777.Groups4Aand4BaredosedwithbothomeprazoleandDMP-777.OnStudyDays1and2,animalsarepretreatedwithomeprazoletwicedaily,thedosingintervalsseparatedbyapproximately6hr.OnStudyDay3(Group4A)orDays3and4(Group4B),omeprazoleiscoadministeredwithDMP-777.Thefirstdoseofomeprazoleisadministeredapproximately1hrpriortothedoseofDMP-777.Theseconddoseisapproximately6hrafterthelastdoseofDMP-777.Groups1A,2A,3A,and4AaresacrificedonDay4.Groups1B,2B,3B,and4BaresacrificedonDay5.Bromodeoxyuridine(BrdU)isadministeredbyintraperitonealinjectiontoalltherats,2hrpriortonecropsy.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•CellStemCell.2022May5;29(5):826-839.e9.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].OgawaM,etal.OmeprazoletreatmentamelioratesoxynticatrophyinducedbyDMP-777.DigDisSci.2006Mar;51(3):431-9.[2].ZagrobelnyJ,etal.Separationofthefourstereoisomersofapotentinhibitor(L-694,458)ofhumanleukocyteelastaseanditsdeterminationinhumanplasmausingachiral/chiralchromatographywithcolumnswitching.JPharmBiomedAnal.1998Sep1;17(6-7[3].WeisVG,etal.Maturityandageinfluencechiefcellabilitytotransdifferentiateintometaplasia.AmJPhysiolGastrointestLiverPhysiol.2016Nov23:ajpg