Ilomastat-GM6001-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIlomastatCat.No.:HY-15768CASNo.:142880-36-2Synonyms:GM6001;Galardin分?式:C??H??N?O?分?量:388.46作?靶點(diǎn):MMP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:≥47mg/mL(120.99mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5743mL12.8713mL25.7427mL5mM0.5149mL2.5743mL5.1485mL10mM0.2574mL1.2871mL2.5743mL請(qǐng)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(qǐng)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(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：0.5%CMC-Na/salinewaterSolubility:10mg/mL(25.74mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.44mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.44mM);Clearsolution4.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.44mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(6.44mM);ClearsolutionBIOLOGICALACTIVITY?物活性Ilomastat(GM6001)?種有效、?譜的質(zhì)?屬蛋?酶(MMP)抑制劑，能夠抑制MMP的活性，IC50值分別為1.5nM(MMP-1)，1.1nM(MMP-2)，1.9nM(MMP-3)，0.5nM(MMP-9)，對(duì)??膚成纖維細(xì)胞膠原酶(MMP-1)的Ki值為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)體外研究Ilomastat(GM6001)inhibitshumanskinfibroblastcollagenase,thermolysinandelastasewithKisof0.4nM,20nM,20nM,resepctively[1].Ilomastat(0.1-10nM)inhibitsgelatinaseAandgelatinaseBproducedbyT-cells.IlomastatinhibitsT-cellhoming[4].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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