Ilomastat-GM6001-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIlomastatCat.No.:HY-15768CASNo.:142880-36-2Synonyms:GM6001;Galardin分⼦式:C₂₀H₂₈N₄O₄分⼦量:388.46作⽤靶点:MMP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:≥47mg/mL(120.99mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5743mL12.8713mL25.7427mL5mM0.5149mL2.5743mL5.1485mL10mM0.2574mL1.2871mL2.5743mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：0.5%CMC-Na/salinewaterSolubility:10mg/mL(25.74mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.44mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.44mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.44mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(6.44mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Ilomastat(GM6001)⼀种有效、⼴谱的质⾦属蛋⽩酶(MMP)抑制剂，能够抑制MMP的活性，IC50值分别为1.5nM(MMP-1)，1.1nM(MMP-2)，1.9nM(MMP-3)，0.5nM(MMP-9)，对⼈⽪肤成纤维细胞胶原酶(MMP-1)的Ki值为0.4nM。IC50&TargetFibroblastcollagenaseMMP-1MMP-2MMP-30.4nM(Ki,Humanskin)1.5nM(IC50)1.1nM(IC50)1.9nM(IC50)MMP-9ThermolysinEastase0.5nM(IC50)20nM(Ki)20nM(Ki)体外研究Ilomastat(GM6001)inhibitshumanskinfibroblastcollagenase,thermolysinandelastasewithKisof0.4nM,20nM,20nM,resepctively[1].Ilomastat(0.1-10nM)inhibitsgelatinaseAandgelatinaseBproducedbyT-cells.IlomastatinhibitsT-cellhoming[4].体内研究Ilomastat(GM6001)(400μg/mL)inhibitscornealulcerationafterseverealkaliinjuryinanimals[2].Ilomastat(GM6001)significantlysuppressesintimalhyperplasiaandintimalcollagencontent.Ilomastatincreaseslumenareainstentedarteries,showsnoactivityonproliferationratesinrabbitmodelafterstenting[3].PROTOCOLAnimalToassesstheeffectsofMMPinhibition,animalsaregivendailyinjectionsofeithervehicle(“placebogroup”)Administration[3]orIlomastat(GM6001)(100mg/kgperdayassubcutaneoussuspension),beginningonedaybeforethesecondinjuryuntilsevendaysaftertheprocedure.Ilomastat(GM6001)isanonspecifichydroxamicacid-basedMMPIwithpotentinhibitoryactivityagainstcollagenase,gelatinasesandstromelysin.Animalsareeuthanizedateither1weekor10weeksafterthesecondinjury.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•NatBiomedEng.2021Jul26.•NatCommun.2017Mar7;8:14483.•JExpMed.2023Feb6;220(2):e20211422.•BioactMater.1February2022.•JAmChemSoc.2021May12;143(18):6847-6854.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GrobelnyD,etal.Inhibitionofhumanskinfibroblastcollagenase,thermolysin,andPseudomonasaeruginosaelastasebypeptidehydroxamicacids.Biochemistry.1992Aug11;31(31):7152-4.[2].SchultzGS,etal.Treatmentofalkali-injuredrabbitcorneaswithasyntheticinhibitorofmatrixmetalloproteinases.InvestOphthalmolVisSci.1992Nov;33(12):3325-31.[3].LiC,etal.ArterialrepairafterstentingandtheeffectsofGM6001,amatrixmetalloproteinaseinhibitor.JAmCollCardiol.2002Jun5;39(11):1852-8.[4].LeppertD,etal.Tcellgelatinasesmediatebasementmembranetransmigrationinvitro.JImmunol.1995May1;154(9):4379-89.[5].YamamotoM,etal.Inhibitionofmembrane-type1matrixmetalloproteinasebyhydroxamateinhibitors:anexaminationofthesubsitepocket.JMedChem.1998Apr9;41(8):1209-17.Mce