ENMD-1068-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEENMD-1068hydrochlorideCat.No.:HY-124748A分?式:C??H??ClN?O?分?量:319.87作?靶點(diǎn):ProteaseActivatedReceptor(PAR);Apoptosis作?通路:GPCR/GProtein;Apoptosis儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:200mg/mL(625.25mM;Needultrasonic)H2O:100mg/mL(312.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1263mL15.6314mL31.2627mL5mM0.6253mL3.1263mL6.2525mL10mM0.3126mL1.5631mL3.1263mL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(storedundernitrogen)。-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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:5mg/mL(15.63mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(15.63mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(15.63mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:100mg/mL(312.63mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性ENMD-1068hydrochloride?種選擇性的蛋?酶激活受體2(PAR2)拮抗劑。ENMD-1068hydrochloride可通過(guò)抑制TGF-β1/Smad信號(hào)轉(zhuǎn)導(dǎo)?減少肝狀細(xì)胞的活化和膠原蛋?的表達(dá)。ENMD-1068hydrochloride還能抑制?宮內(nèi)膜細(xì)胞的增殖，并誘導(dǎo)病灶中上?細(xì)胞的凋亡。ENMD-1068hydrochloride可?于?宮內(nèi)膜異位癥、肝纖維化的研究。IC50&TargetPAR2體外研究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(?),Colα1(III),andSmad2/3C-terminalphosphorylation.體內(nèi)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?邊的抑制劑?師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