PHA-568487-free-base-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPHA568487freebaseCat.No.:HY-129674CASNo.:527680-56-4分?式:C??H??N?O?分?量:288.34作?靶點(diǎn):nAChR作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(86.70mM;ultrasonicandwarmingandadjustpHto8withHClandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.4681mL17.3406mL34.6813mL5mM0.6936mL3.4681mL6.9363mL10mM0.3468mL1.7341mL3.4681mL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。-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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.21mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.21mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.21mM);ClearsolutionBIOLOGICALACTIVITY?物活性PHA568487freebase?種選擇性的α7煙堿?酰膽堿受體(α-7nAchR)激動(dòng)劑。PHA568487freebase可?于減緩神經(jīng)炎癥。體外研究PHA568487,α-7nAchR-specificagonist,preventsNF-κbactivationinthecells[2].PHA568487treatmentsignificantlyreducestheexpressionofleukocyteinfiltrationmoleculesinMCAOratsandinendothelialcellsafterinvitroischemia[3].體內(nèi)研究PHA568487treatmentreducesmousecognitivedeclinecausedbyasepticbonefracturebypromotinginflammationresolution.PHA568487(PHA;0.8mg/kg;injectedintraperitoneally)reducesinfarctvolumeandTUNELpositiveneuronsintheperi-infarctregionsofpermanentmiddlecerebralarteryocclusion(pMCAO)andpMCAO+tibiafracturemice[2].Theroleplayedbya7receptorsonneuroinflammationissupportedbythedecreaseof[18F]DPA-714bindinginischemicratstreatedwiththea7agonistPHA568487atday7afterMCAO[3].PHA568487-treatedischemicratsshowasignificantreductionofthecerebralinfarctvolumesandanimprovementoftheneurologicoutcomecomparedwithnon-treatedMCAOrats[3].AnimalModel:C57BL/6Jmalemice(10-12weeksold)withpMCAO[2]Dosage:0.4and0.8mg/kgAdministration:Injectedintraperitoneallyonceonday1,ortwiceondays1and2,afterpMCAOResult:0.8mg/kgondays1and2afterpMCAOyieldedthebesteffectoninfarctvolumeandbehaviortests.AnimalModel:AdultmaleSprague-Dawleyrats[3]Dosage:1.25mg/kgAdministration:Treatedi.p.dailywith0.1mLResult:Showedasignificantdecreaseof[18F]DPA-714bindingintheischemiccerebralhemisphereincomparisontonon-treatedischemicrats.REFERENCES[1].FBarclayShilliday,etal.MultiplespeciesmetabolismofPHA-568487,aselectivealpha7nicotinicacetylcholinereceptoragonist.Drug2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMetabLett.2010Aug;4(3):162-72.[2].ZhenyingHan,etal.Alpha-7nicotinicacetylcholinereceptoragonisttreatmentreducesneuroinflammation,oxidativestress,andbraininjuryinmicewithischemicstrokeandbonefracture.JNeurochem.2014Nov;131(4):498-508.[3].LorenaColás,etal.InvivoimagingofΑ7nicotinicreceptorsasanovelmethodtomonitorneuroinflammationaftercerebralischemia.Glia.2018Aug;66(8):1611-1624.McePdfHeightCaution:Producthasno