PZ-128-P1pal-7-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPZ-128Cat.No.:HY-107146CASNo.:371131-16-7Synonyms:P1pal-7分?式:C??H??N??O?分?量:1086.46SequenceShortening:{Palmitate}-KKSRALF-NH2作?靶點(diǎn):ProteaseActivatedReceptor(PAR)作?通路:GPCR/GProtein儲(chǔ)存?式:Powder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(92.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.9204mL4.6021mL9.2042mL5mM0.1841mL0.9204mL1.8408mL10mM0.0920mL0.4602mL0.9204mL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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.30mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(2.30mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.30mM);ClearsolutionBIOLOGICALACTIVITY?物活性PZ-128(P1pal-7)?種細(xì)胞穿透肽，?種?創(chuàng)的，特異性的且可逆的蛋?酶激活受體1(PAR1)拮抗劑。PZ-128靶向PAR1的細(xì)胞質(zhì)表，并中斷向內(nèi)部定位G(PAR1-G)蛋?的信號(hào)。PZ-128具有抗??板，抗轉(zhuǎn)移，抗?管?成和抗癌作?。體外研究PZ-128(P1pal-7;3μM)blocks90-94%ofOVCAR-4migrationtowardhumanovarianascitesandfibroblastconditionedmedia.TheOVCAR4-treatedperitonealfibroblastconditionedmediaelicitsa2.2-foldincreaseinendothelialbarrierpermeabilitywhichcouldbenearlycompletelyinhibitedbyPZ-128[1].PZ-128isalipidated‘pepducin’whichtargetsthecytoplasmicsurfaceofPAR1andinterruptssignalingtointernally-locatedGproteins.ThestructureofPZ-128isfoundtomimictheoff-stateofthecorrespondingintracellularregionofPAR1whichiscriticalforcouplingtoGproteins[3].體內(nèi)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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfu