PFE-360-PF-06685360-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPFE-360Cat.No.:HY-120085CASNo.:1527475-61-1Synonyms:PF-06685360分?式:C??H??N?O分?量:308.34作?靶點:LRRK2作?通路:Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:10.42mg/mL(33.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2432mL16.2159mL32.4317mL5mM0.6486mL3.2432mL6.4863mL10mM0.3243mL1.6216mL3.2432mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1.04mg/mL(3.37mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.04mg/mL(3.37mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.04mg/mL(3.37mM);ClearsolutionBIOLOGICALACTIVITY?物活性PFE-360(PF-06685360)有效的、選擇性的、能透過?腦屏障的、?服有效的LRRK2的抑制劑，體內(nèi)測得的平均IC50值為2.3nM。IC50&TargetIC50:2.3nM(LRRK2invivo)[1][2].體內(nèi)研究PFE-360(4mg/kgand7.5mg/kg,orally,BID,10-12weeks)treatmentpotentlydecreasestheLRRK2-pSer935/totalLRRK2ratio,withnosignificantadverseeffects[1].AnimalModel:FemaleSpragueDawleyrats(NTac:SD)weighed225-250g[3].Dosage:4mg/kgand7.5mg/kg(pharmacokineticsandpharmacodynamics).Administration:OrallyBIDfor10-12weeks.Result:TheLRRK2-pSer935/totalLRRK2ratiowassignificantlydecreasedatboth1hand12hafterdosing.Theterminalbodyweightsexhibitednosignificantchanges.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?StemCellReports.2022Sep12;S2213-6711(22)00423-4.?FrontCellDevBiol.2020Oct28;8:594090.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MarcoA.S.Baptista,etal.LRRK2KinaseInhibitorsofDifferentStructuralClassesInduceAbnormalAccumulationofLamellarBodiesinTypeIIPneumocytesinNon-HumanPrimatesbutareReversibleandWithoutPulmonaryFunctionalConsequences.[2].AndersenMA,etal.Parkinson'sdisease-likeburstfiringactivityinsubthalamicnucleusinducedbyAAV-α-synucleinisnormalizedbyLRRK2modulation.NeurobiolDis.2018Aug;116:13-27.[3].AndersenMA,etal.PFE-360-inducedLRRK2inhibitioninducesreversible,non-adverserenalchangesinrats.Toxicology.2018Feb15;395:15-22.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplica