Tirofiban-hydrochloride-L700462-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETirofibanhydrochlorideCat.No.:HY-17369ACASNo.:142373-60-2Synonyms:L700462hydrochloride;MK383hydrochloride分?式:C??H??ClN?O?S分?量:477.06作?靶點(diǎn):Integrin作?通路:Cytoskeleton儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Tirofiban(L700462)hydrochloride?種選擇性和可逆性的??板整合素受體(GpIIb/IIIa)拮抗劑，能抑制纖維蛋?原與該受體結(jié)合，具有抗?栓活性。Tirofibanhydrochloride可通過誘導(dǎo)VEGF的產(chǎn)?來(lái)刺激內(nèi)?細(xì)胞的遷移和增殖。Tirofibanhydrochloride可通過緩解缺?區(qū)的?肌微?管結(jié)構(gòu)和內(nèi)?功能障礙顯著減少?肌?回流和缺?再灌注損傷，從?改?臟功能。IC50&TargetGpIIb/IIIareceptor[1].體外研究Tirofibanhydrochloride(0.25,1,3μg/mL;72hours)increasesproliferationofHAECcells[1].Tirofibanhydrochloride(24hours)closesthescratchofHUVECsmigrationwithin18hours[1].Tirofibanhydrochloride(0.25,1μg/mL;1hour)inducesproductionofVEGFafter30minuteswhichcanstimulatesproliferationofendothelialcells[1].CellProliferationAssay[1]CellLine:HAECcellsConcentration:0.25,1,3μg/mLIncubationTime:72hoursResult:IncreasedproliferationofHAECcells.CellMigrationAssay[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:HUVECcellsConcentration:IncubationTime:24hoursResult:Stimulatedthemigratorycapacityofendothelialcells.WesternBlotAnalysis[1]CellLine:HAECcellsConcentration:0.05,0.12,0.25,1μg/mLIncubationTime:1hourResult:InducedproductionofVEGFwhichstimulatedproliferationofendothelialcells.體內(nèi)研究Tirofibanhydrochloride(60μg/kg;i.v.;once)showsactivityofincreasingcontractionforce,ventricularcompliance,andimprovingheartfunctionbyincreasingHR,LVESP,dp/dtmax,andreducingLVEDP[2].Tirofibanhydrochloride(60μg/kg;i.v.;once)enhanceseNOSactivity,decreasesiNOSactivityandreducesareaofno-reflowafterreperfusionfollowingAMI[2].Tirofibanhydrochloride(50μg/per;irrigate;once)showsanticoagulanteffectwithpatencyratesof59%at24hoursaftermicrovascularanastomosisinthecrushmodel[3].AnimalModel:MaleSprague-Dawleyrats(10to15-week-age;270-330g)[2].Dosage:60μg/kgAdministration:Intravenousinjection;once.Result:Increasedcontractionforce,ventricularcompliance,andimprovedheartfunction.Reducedthesizeofno-reflowandinfarct.AnimalModel:Sprague-Dawleyrats(350-400g;crushinjurymodel)[3]Dosage:50μg/per(50μg/mL,1mLforeach)Administration:Irrigate1mLwithinthevessellumen(beforeplacementofthelastsuture);once.Result:Showedanticoagulanteffectwithpatencyratesof59%.REFERENCES[1].GiordanoA,etal.TirofibaninducesVEGFproductionandstimulatesmigrationandproliferationofendothelialcells.VasculPharmacol.2014May-Jun;61(2-3):63-71.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].LiuX,etal.Effectsoftirofibanonthereperfusion-relatedno-reflowinratswithacutemyocardialinfarction.JGeriatrCardiol.2013Mar;10(1):52-8.[3].YatesYJ,etal.Theeffectoftirofibanonmicrovascularthrombosis:crushmodel.PlastReconstrSurg.2005Jul;116(1):205-8.McePdfHeightCaution:Producthasnotbeenfullyvalida