PD-117519-CI947-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPD117519Cat.No.:HY-100032CASNo.:96392-15-3Synonyms:CI947分⼦式:C₁₉H₂₁N₅O₄分⼦量:383.4作⽤靶点:AdenosineReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(260.82mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6082mL13.0412mL26.0824mL5mM0.5216mL2.6082mL5.2165mL10mM0.2608mL1.3041mL2.6082mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.52mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.52mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PD117519(CI947)⼀种A2A腺苷激动剂，在药理动物模型中具有⼝服降压活性。IC50&TargetA2Aadenosine[1]体内研究PD117519(2-10mg/kg;oraladministration;16-24hours;malebeagledogs)treatmentproducessignificanthemodynamicchangesatTmax(4hours)followsbyacutecoronaryvascularinjurythatisevidentat16hourspostdosing.Treatmentwith2or10mg/kgofPD117519producessignificantincreasesinmeanheartrateanddecreasesinmeanindirectsystolicbloodpressureattimeofhighestdrugexposure,4hourspostdosing[3].AnimalModel:24malebeagledogs(8-12monthsold)[3]Dosage:2mg/kgor10mg/kgAdministration:Oraladministration;16hoursand24hoursResult:Increasedinmeanheartrateanddecreasedinmeanindirectsystolicbloodpressureattimeofhighestdrugexposure.Inducedacutecoronaryarteriopathy.Theendotheliumalsoappearsinjured.REFERENCES[1].ReynoldsDL,etal.LiquidchromatographicanalysisoftheadenosineagonistPD117519indogplasma.JPharmBiomedAnal.1991;9(4):345-9.[2].TobinGA,etal.TheroleofeNOSphosphorylationincausingdrug-inducedvascularinjury.ToxicolPathol.2014Jun;42(4):709-24.[3].EnersonBE,etal.Acutedrug-inducedvascularinjuryinbeagledogs:pathologyandcorrelatinggenomicexpression.ToxicolPathol.2006;34(1):27-32.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forres