Cl-amidine-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECl-amidinehydrochlorideCat.No.:HY-100574ACASNo.:1373232-26-8分⼦式:C₁₄H₂₀Cl₂N₄O₂分⼦量:347.24作⽤靶点:ProteinArginineDeiminase;Apoptosis;MicroRNA作⽤通路:Epigenetics;Apoptosis储存⽅式:-20°C,storedundernitrogen,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(287.99mM;Needultrasonic)H2O:50mg/mL(143.99mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8799mL14.3993mL28.7985mL5mM0.5760mL2.8799mL5.7597mL10mM0.2880mL1.4399mL2.8799mL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,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：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥7.5mg/mL(21.60mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥7.5mg/mL(21.60mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥7.5mg/mL(21.60mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:5.5mg/mL(15.84mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Cl-amidinehydrochloride⼝服有效的PAD抑制剂，其对PAD1、PAD3和PAD4的IC50值分别为0.8μM、6.2μM和5.9μM。Cl-amidinehydrochloride可诱导癌细胞的凋亡。Cl-amidinehydrochloride可诱导miR-16(miRNA-16,microRNA-16)，引起细胞周期阻滞。Cl-Amidinehydrochloride可阻断组蛋⽩3⽠氨酸化和中性粒细胞胞外陷阱的形成，并提⾼败⾎症⼩⿏的存活率。IC50&TargetIC50:0.8μM(PAD1),5.9μM(PAD4),6.2μM(PAD3)[1][5].体外研究Cl-amidineisabioavailablehaloacetamidine-basedcompoundthatinhibitsalltheactivePADisozymeswithnearequalpotency(kinact/KI=13,000M-1•min-1forPAD4)[1].Cl-amidine(0,5,10,15,20,25,50μg/mL,24hours)inducesapoptosisinTK6lymphoblastoidcellsandHT29coloncancercellsinadose-dependentmanner.Interestingly,thecoloncancercellline(HT29)isrelativelyresistanttoapoptosiscausedbyCl-amidine[2].Cl-Amidinepreventshistone3citrullinationandneutrophilextracellulartrapformation,andimprovessurvivalinamurinesepsismodel[4].ApoptosisAnalysis[2].CellLine:TK6lymphoblastoidcellsandHT29coloncancercells.Concentration:0,5,10,15,20,25,50μg/mL.IncubationTime:24h.Result:Inducedapoptosisdose-dependently.体内研究Cl-amidine(75mg/kg,iponcedaily)suppressesandtreatsDSS-inducedcolitisinmice[2].Cl-amidine(5,25,75mg/kg,oralgavage,oncedaily)leadstosignificantreductionsinthehistologyscoresdose-dependently[2].AnimalModel:C57BL/6mice(8-12wkold,DSSmousemodelofcolitis)[2].Dosage:75mg/kg.Administration:IPoncedaily.Result:SuppressedPADactivity,proteincitrullination,andPADlevelsinthecoloninvivo.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:C57BL/6mice(8-12wkold,DSSmousemodelofcolitis)[2].Dosage:5,25,75mg/kg.Administration:Oralgavageoncedaily.Result:Ledtosignificantreductionsinthehistologyscores.户使⽤本产品发表的科研⽂献•TranslRes.2022Nov23;S1931-5244(22)00252-3.•CellRep.2021Sep21;36(12):109750.•Neoplasia.2022Nov;33:100835.•FishShellfishImmunol.2022Aug3;S1050-4648(22)00414-4.•ChemResToxicol.2022Feb15.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YuanLuo,etal.InhibitorsandInactivatorsofProteinArginineDeiminase4:FunctionalandStructuralCharacterization.Biochemistry.2006Oct3;45(39):11727–11736.[2].ChumanevichAA,etal.SuppressionofcolitisinmicebyCl-amidine:anovelpeptidylargininedeiminaseinhibitor.AmJPhysiolGastrointestLiverPhysiol.2011Jun;300(6):G929-38.[3].WitalisonEE,etal.Moleculartargetingofproteinargininedeiminasestosuppresscolitisandpreventcoloncancer.Oncotarget.2015Nov3;6(34):36053-62.[4].BironBM,etal.,Cl-AmidinePreventsHistone3CitrullinationandNeutrophilExtracellularTrapFormation,andImprovesSurvivalinaMurineSepsisModel.JInnateImmun.2017;9(1):22