URB-597-KDS-4103-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEURB-597Cat.No.:HY-10864CASNo.:546141-08-6Synonyms:KDS-4103分?式:C??H??N?O?分?量:338.4作?靶點:FAAH;Autophagy;Mitophagy作?通路:MetabolicEnzyme/Protease;NeuronalSignaling;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:≥100mg/mL(295.51mM)H2O:0.1mg/mL(0.30mM;ultrasonicandwarmingandheatto50°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9551mL14.7754mL29.5508mL5mM0.5910mL2.9551mL5.9102mL10mM0.2955mL1.4775mL2.9551mL請根據產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，避免反復凍融造成的產品失效。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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、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%salineSolubility:10mg/mL(29.55mM);Clearsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.39mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.39mM);ClearsolutionBIOLOGICALACTIVITY?物活性URB-597(KDS-4103)?種有效的，具有?服活性的選擇性FAAH抑制劑。URB-597抑制??腦膜中FAAH活性，IC50為5nM，抑制體外??神經元中FAAH活性，IC50為0.5nM，抑制?肝微粒體中FAAH活性，IC50為3nM。具有抗抑郁樣作?，可?于緩解疼痛的研究[1]。體外研究URB-597(KDS-4103)preventstheFAAH-catalyzedhydrolysisof[3H]anandamidebyprimaryculturesofratcorticalneuronswithanIC50valueof~0.50nM[1].體內研究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.戶使?本產品發(fā)表的科研?獻?OxidMedCellLongev.2022May12;2022:4139330.?CerebCortex.2020Dec21;bhaa363.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].DanielePiomelli,etal.PharmacologicalprofileoftheselectiveFAAHinhibitorKDS-4103(URB597).CNSDrugRev.Spring2006;12(1):21-38.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform