URB-597-KDS-4103-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEURB-597Cat.No.:HY-10864CASNo.:546141-08-6Synonyms:KDS-4103分⼦式:C₂₀H₂₂N₂O₃分⼦量:338.4作⽤靶点:FAAH;Autophagy;Mitophagy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(295.51mM)H2O:0.1mg/mL(0.30mM;ultrasonicandwarmingandheatto50°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9551mL14.7754mL29.5508mL5mM0.5910mL2.9551mL5.9102mL10mM0.2955mL1.4775mL2.9551mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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%salineSolubility:10mg/mL(29.55mM);Clearsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.39mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.39mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性URB-597(KDS-4103)⼀种有效的，具有⼝服活性的选择性FAAH抑制剂。URB-597抑制⼤⿏脑膜中FAAH活性，IC50为5nM，抑制体外⼤⿏神经元中FAAH活性，IC50为0.5nM，抑制⼈肝微粒体中FAAH活性，IC50为3nM。具有抗抑郁样作⽤，可⽤于缓解疼痛的研究[1]。体外研究URB-597(KDS-4103)preventstheFAAH-catalyzedhydrolysisof[3H]anandamidebyprimaryculturesofratcorticalneuronswithanIC50valueof~0.50nM[1].体内研究URB-597(KDS-4103)inhibitsratbrainFAAHactivityafterintraperitoneal(i.p.)administrationwithamedianinhibitorydose(ID50)of0.15mg/kginwild-typemice(+/+)orFAAH-nullmice(-/-)[1].KDS-4103(0.1-0.3mg/kg,i.p.)elicitssignificant,anxiolytic-like,antidepressant-likeandanalgesiceffects,whicharepreventedbytreatmentwithCB1receptorantagonistsinratsandmice[1].KDS-4103isorallyavailableinratsandcynomolgusmonkeys[1].URB-597inhibitsFAAHinthebrainrapidly(1h),sustainsat>90%through12hand>60%through24hafteranoraldoseof10mg/kg.AnimalModel:Wistarrats[1]Dosage:250,500,750,1000,1250mg/kg(PharmacokineticAnalysis)Administration:OraladministrationResult:Absorbedatamoderateratewithpeakplasmaconcentrations(Cmax)achievedat1.2haftertreatment.Theoraleliminationhalf-lifewasapproximately2h.户使⽤本产品发表的科研⽂献•OxidMedCellLongev.2022May12;2022:4139330.•CerebCortex.2020Dec21;bhaa363.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].DanielePiomelli,etal.PharmacologicalprofileoftheselectiveFAAHinhibitorKDS-4103(URB597).CNSDrugRev.Spring2006;12(1):21-38.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform