PZ-128-P1pal-7-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPZ-128Cat.No.:HY-107146CASNo.:371131-16-7Synonyms:P1pal-7分⼦式:C₅₅H₉₉N₁₃O₉分⼦量:1086.46SequenceShortening:{Palmitate}-KKSRALF-NH2作⽤靶点:ProteaseActivatedReceptor(PAR)作⽤通路:GPCR/GProtein储存⽅式:Powder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(92.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9204mL4.6021mL9.2042mL5mM0.1841mL0.9204mL1.8408mL10mM0.0920mL0.4602mL0.9204mL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)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.30mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(2.30mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.30mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PZ-128(P1pal-7)⼀种细胞穿透肽，⼀种⾸创的，特异性的且可逆的蛋⽩酶激活受体1(PAR1)拮抗剂。PZ-128靶向PAR1的细胞质表，并中断向内部定位G(PAR1-G)蛋⽩的信号。PZ-128具有抗⾎⼩板，抗转移，抗⾎管⽣成和抗癌作⽤。体外研究PZ-128(P1pal-7;3μM)blocks90-94%ofOVCAR-4migrationtowardhumanovarianascitesandfibroblastconditionedmedia.TheOVCAR4-treatedperitonealfibroblastconditionedmediaelicitsa2.2-foldincreaseinendothelialbarrierpermeabilitywhichcouldbenearlycompletelyinhibitedbyPZ-128[1].PZ-128isalipidated‘pepducin’whichtargetsthecytoplasmicsurfaceofPAR1andinterruptssignalingtointernally-locatedGproteins.ThestructureofPZ-128isfoundtomimictheoff-stateofthecorrespondingintracellularregionofPAR1whichiscriticalforcouplingtoGproteins[3].体内研究PZ-128(P1pal-7;10mg/kg;intraperitonealinjection;everyotherday;for6weeks)treatmentsignificantlyreducesmeanascitesfluidvolumeby60%.PZ-128treatmentalsocausesahighlysignificant84-96%reductioninbloodvesseldensityinboththecenterandedgeoftheOVCAR-4tumors[1].AnimalModel:FemaleNCRNu/Numice(5-7weeks)injectedwithOVCAR-4orSKOV-3cells[1]Dosage:10mg/kgAdministration:Intraperitonealinjection;everyotherday;for6weeksResult:Significantlyreducedmeanascitesfluidvolumeby60%.REFERENCES[1].AnikaAgarwal,etal.Targetingametalloprotease-PAR1signalingsystemwithcell-penetratingpepducinsinhibitsangiogenesis,ascites,andprogressionofovariancancer.MolCancerTher.2008Sep;7(9):2746-57.[2].LidijaCovic,etal.Protease-ActivatedReceptor1asTherapeuticTargetinBreast,Lung,andOvarianCancer:PepducinApproach.IntJMolSci.2018Jul31;19(8):2237.[3].PaulAGurbel,etal.Cell-PenetratingPepducinTherapyTargetingPAR1inSubjectsWithCoronaryArteryDisease.ArteriosclerThrombVascBiol.2016Jan;36(1):189-97.[4].PingZhang,etal.Suppressionofarterialthrombosiswithoutaffectinghemostaticparameterswithacell-penetratingPAR1pepducin.Circulation.2012Jul3;126(1):83-91.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfu