Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENampt-IN-5Cat.No.:HY-130606CASNo.:2380013-17-0分?式:C??H??N?O?分?量:427.5作?靶點:NAMPT;CytochromeP450作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:50mg/mL(116.96mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3392mL11.6959mL23.3918mL5mM0.4678mL2.3392mL4.6784mL10mM0.2339mL1.1696mL2.3392mL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?現配，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沉淀、析出現象，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:≥2.5mg/mL(5.85mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性Nampt-IN-5?種有效的煙酰胺磷酸核糖轉移酶(NAMPT)抑制劑。Nampt-IN-5還抑制CYP3A4活性。Nampt-IN-5可抑制A2780和COR-L23細胞，IC50值分別為0.7nM和3.9nM。IC50&TargetNAMPT[1]CYP3A4[1]體外研究Nampt-IN-5(compound27)(0-10nM;3days)hascellularIC50sof0.7nMand3.9nMagainstA2780andCOR-L23,respectively[1].Nampt-IN-5showsagoodADMEdata:mousemicrosomalclearance(110μl/min?mg),CYP3A4inhibitionvalue(0.75μM),Sol6.8:0.056mM;MDCKPappAB:18.6[1].體內研究Nampt-IN-5(5-30mg/kg;p.o.twicedailyfor4days)causesasignificantamountofbodyweightlossinnudemicerelativetovehicle[1].Nampt-IN-5(10mg/kg;p.o.)exhibitsT1/2(2.1h),Cmax(29112nM),andAUC(61984nM?h)inmice[1].REFERENCES[1].PalaciosDS,etal.ScaffoldMorphingIdentifies3-PyridylAzetidineUreasasInhibitorsofNicotinamidePhosphoribosyltransferase(NAMPT).ACSMedChemLett.2019Oct10;10(11):1524-1529.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40