ENMD-1068-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEENMD-1068hydrochlorideCat.No.:HY-124748A分⼦式:C₁₅H₃₀ClN₃O₂分⼦量:319.87作⽤靶点:ProteaseActivatedReceptor(PAR);Apoptosis作⽤通路:GPCR/GProtein;Apoptosis储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:200mg/mL(625.25mM;Needultrasonic)H2O:100mg/mL(312.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1263mL15.6314mL31.2627mL5mM0.6253mL3.1263mL6.2525mL10mM0.3126mL1.5631mL3.1263mL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:5mg/mL(15.63mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(15.63mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(15.63mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:100mg/mL(312.63mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性ENMD-1068hydrochloride⼀种选择性的蛋⽩酶激活受体2(PAR2)拮抗剂。ENMD-1068hydrochloride可通过抑制TGF-β1/Smad信号转导⽽减少肝状细胞的活化和胶原蛋⽩的表达。ENMD-1068hydrochloride还能抑制⼦宫内膜细胞的增殖，并诱导病灶中上⽪细胞的凋亡。ENMD-1068hydrochloride可⽤于⼦宫内膜异位症、肝纤维化的研究。IC50&TargetPAR2体外研究ENMD-1068(10mM;24h)blocksTGF-β1/SmadsignalinginprimarymouseHSCs(TGF-β1/SmadsignalpathwayplaysacrucialroleinHSCsactivationandcollagenproduction)[1].ENMD-1068(10mM)inhibitstrypsinorSLIGRL-NH2stimulatedcalciumreleaseinHSCs[1].WesternBlotAnalysis[1]CellLine:Hepaticstellatecells(HSCs)(TGF-β1-stimulated)Concentration:10mMIncubationTime:24hResult:InhibitedTGF-β1-inducedexpressionofα-SMA,Colα1(І),Colα1(III),andSmad2/3C-terminalphosphorylation.体内研究ENMD-1068(25,50mg/kg;i.p.;twiceperweekfor4weeks)inhibitsliverfibrosisofmice[1].ENMD-1068(25,50mg/kg;i.p.;singledailyfor5days)inhibitsendometriosisgrowthandsuppressesthelevelsofIL-6andMCP-1inadose-dependentmanner[2].ENMD-1068(25,50mg/kg;i.p.;singledailyfor5days)causesadecreaseinepithelialcellproliferationandanincreaseintheapoptoticindexinmice[2].AnimalModel:ICRmice(8-week-old;CCl4-inducedliverfibrosismodel)[1].Dosage:25,50mg/kgAdministration:Intraperitonealinjection;twiceperweekfor4weeksResult:Markedlyattenuatedcollagendeposition.AnimalModel:Micewithsurgicallyinducedendometriosis[2].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:25,50mg/kgAdministration:Intraperitonealinjection;singledailyfor5daysResult:Reducedthevolumeofobservedlesionsinadose-dependentmanner.InhibitedtheexpressionofIL-6andMCP-1.Decreasedtheproliferationrateofendometrioticcellsandincreasedthepercentageofapoptoticepithelialcellsinthelesions.REFERENCES[1].SunQ,etal.ENMD-1068inhibitsliverfibrosisthroughattenuationofTGF-β1/Smad2/3signalinginmice.SciRep.2017Jul14;7(1):5498.doi:10.1038/s41598-017-05190-7.Erratumin:SciRep.2019Dec10;9(1):19125.[2].WangY,etal.ENMD-1068,aprotease-activatedreceptor2antagonist,inhibitsthedevelopmentofendometriosisinamousemodel.AmJObstetGynecol.2014Jun;210(6):531.e1-8.McePdfHeightCaution:Product