PFE-360-PF-06685360-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPFE-360Cat.No.:HY-120085CASNo.:1527475-61-1Synonyms:PF-06685360分⼦式:C₁₆H₁₆N₆O分⼦量:308.34作⽤靶点:LRRK2作⽤通路:Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:10.42mg/mL(33.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2432mL16.2159mL32.4317mL5mM0.6486mL3.2432mL6.4863mL10mM0.3243mL1.6216mL3.2432mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.04mg/mL(3.37mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.04mg/mL(3.37mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.04mg/mL(3.37mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PFE-360(PF-06685360)有效的、选择性的、能透过⾎脑屏障的、⼝服有效的LRRK2的抑制剂，体内测得的平均IC50值为2.3nM。IC50&TargetIC50:2.3nM(LRRK2invivo)[1][2].体内研究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.户使⽤本产品发表的科研⽂献•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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplica