PF-3845-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPF-3845Cat.No.:HY-14380CASNo.:1196109-52-0分⼦式:C₂₄H₂₃F₃N₄O₂分⼦量:456.46作⽤靶点:FAAH;Autophagy作⽤通路:MetabolicEnzyme/Protease;NeuronalSignaling;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(219.08mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1908mL10.9539mL21.9077mL5mM0.4382mL2.1908mL4.3815mL10mM0.2191mL1.0954mL2.1908mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.48mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.48mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.48mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PF-3845⼀种有效的，选择性的，不可逆和具有⼝服活性的脂酸酰胺⽔解酶(FAAH)抑制剂，Ki值为0.23µM。PF-3845将FAAH的丝氨酸亲核试剂氨甲酸酯化的共价抑制剂。PF-3845可以减少疼痛感，炎症和焦虑/抑郁，⽽对运动或认知没有实质性响。IC50&TargetKi:0.23µM(FAAH)[1]体外研究PF-3845(0.5nM-10μM;40min)inhibitshumanFAAH-1(IC50=18nM)inaconcentration-dependentmanner,andshowsnegligibleactivityagainstFAAH-2(IC50>10μM)inCOS-7cells[1].PF-3845(0.1-1000μM;48h)significantlydecreasestheColo-205cellviability[2].体内研究PF-3845(1-30mg/kg;p.o.)producescannabinoidreceptor-dependentreductionsininflammatorypaininrat[1].PF-3845(10mg/kg;asinglei.p.)selectivelyinhibitsFAAHinmiceforupto24hours[1].PF-3845(10mg/kg;asinglei.p.)causesadramaticandsustainedelevationinAnandamide(AEA)inmice[1].AnimalModel:MaleSprague-Dawleyrats(200g-250g)areinjectedCFA[1]Dosage:1,3,10,30mg/kgAdministration:OraladministrationResult:Causedadose-dependentinhibitionofmechanicalallodyniawithaminimumeffectivedose(MED)of3mg/kg.户使⽤本产品发表的科研⽂献•CellDeathDiffer.2022Sep14.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AhnK,etal.DiscoveryandcharacterizationofahighlyselectiveFAAHinhibitorthatreducesinflammatorypain.ChemBiol.2009Apr24;16(4):411-20.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].BookerL,etal.Thefattyacidamidehydrolase(FAAH)inhibitorPF-3845actsinthenervoussystemtoreverseLPS-inducedtactileallodyniainmice.BrJPharmacol,2012,165(8),2485-2496.[3].WasilewskiA,et,al.Fattyacidamidehydrolase(FAAH)inhibitorPF-3845reducesviability,migrationandinvasivenessofhumancolonadenocarcinomaColo-205cellline:aninvitrostudy.ActaBiochimPol.2017;64(3):519-525.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo