PD-117519-CI947-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPD117519Cat.No.:HY-100032CASNo.:96392-15-3Synonyms:CI947分?式:C??H??N?O?分?量:383.4作?靶點(diǎn):AdenosineReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(260.82mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6082mL13.0412mL26.0824mL5mM0.5216mL2.6082mL5.2165mL10mM0.2608mL1.3041mL2.6082mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.52mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.52mM);ClearsolutionBIOLOGICALACTIVITY?物活性PD117519(CI947)?種A2A腺苷激動劑，在藥理動物模型中具有?服降壓活性。IC50&TargetA2Aadenosine[1]體內(nèi)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