PF-04418948-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPF-04418948Cat.No.:HY-18966CASNo.:1078166-57-0分?式:C??H??FNO?分?量:409.41作?靶點:ProstaglandinReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:130mg/mL(317.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4425mL12.2127mL24.4254mL5mM0.4885mL2.4425mL4.8851mL10mM0.2443mL1.2213mL2.4425mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.11mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.11mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.11mM);Clearsolution4.請依序添加每種溶劑：2%DMSO>>40%PEG300>>5%Tween-80>>53%salineSolubility:≥2.6mg/mL(6.35mM);Clearsolution5.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥6.5mg/mL(15.88mM);ClearsolutionBIOLOGICALACTIVITY?物活性PF-04418948?種有具有?服活性，有效且選擇性的前列腺素EP2受體拮抗劑，IC50為16nM。體外研究PF-04418948(2μM;90min)inhibitsprostaglandinE2(PGE2)-inducedincreaseincAMP[1].CellViabilityAssay[1]CellLine:CHOcellsConcentration:2μMIncubationTime:90minResult:InhibitedprostaglandinE2(PGE2)-inducedincreaseincAMPincellsexpressingEP2receptorswithafunctionalKBvalueof1.8nM.體內(nèi)研究PF-04418948(oralgavage;1,3,and10mg/kg;once)attenuatsthebutaprost-inducedcutaneousbloodflowresponse[1].AnimalModel:SpragueDawleyrats[1]Dosage:1,3,and10mg/kgAdministration:Oralgavage;1,3,and10mg/kg;onceResult:ReducedthepeakandAUCbutaprost-inducedcutaneousbloodflowresponseinadose-dependentfashion.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?BrainBehavImmun.2021Sep6;98:337-348.?JVirol.2018Sep26;92(20):e01018-18.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].afForsellesKJ,etal.InvitroandinvivocharacterizationofPF-04418948,anovel,potentandselectiveprostaglandinEP2receptorantagonist.BrJPharmacol.2011Dec;164(7):1847-1856.[2].BirrellMA,etal.SelectivityprofilingofthenovelEP2receptorantagonist,PF-04418948,infunctionalbioassaysystems:atypicalaffinityattheguineapigEP2receptor.BrJPharmacol.2013Jan;168(1):129-138.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap