Benzylacyclouridine-BAU-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBenzylacyclouridineCat.No.:HY-106406CASNo.:82857-69-0Synonyms:BAU;5-Benzylacyclouridine分⼦式:C₁₄H₁₆N₂O₄分⼦量:276.29作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(361.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.6194mL18.0969mL36.1939mL5mM0.7239mL3.6194mL7.2388mL10mM0.3619mL1.8097mL3.6194mL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:≥2.5mg/mL(9.05mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.05mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.05mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Benzylacyclouridine(BAU)⼀种有效且特异性的尿苷磷酸化酶抑制剂，尿苷磷酸化酶尿苷分解代谢中的第⼀种酶。Benzylacyclouridine可以调节5-氟尿嘧啶(5-FU)及其衍⽣物的细胞毒副作⽤。IC50&Targeturidinephosphorylase[1]体外研究Benzylacyclouridineincreases5-FU-inducedcytotoxicityinanumberofhumancancercelllines[1].Benzylacyclouridine(20-100μM)reducestherapidclearanceoftraceamountsofeither[14C]uridineorhyperphysiologicconcentrationsofnon-labeleduridinebytheisolatedratliverperfusedwithanartificialoxygencarrier[2].体内研究Benzylacyclouridine(p.o.ori.v.)arreststherapiddegradationofatracerdoseofuridineintouracilindogsandpigs[1].Benzylacyclouridineexhibitsthet1/2of1.8-3.6hindogs,withbioavailabilitylevelsof85%(30mg/kg)and42.5%(120mg/kg)[1].Benzylacyclouridine(120mg/kg)exhibitsthet1/2of1.6-2.3h,withabioavailabilityof40%inpigs[1].REFERENCES[1].PizzornoG,et,al.PhaseIclinicalandpharmacologicalstudiesofbenzylacyclouridine,auridinephosphorylaseinhibitor.ClinCancerRes.1998May;4(5):1165-75.[2].RoosildTP,et,al.Implicationsofthestructureofhumanuridinephosphorylase1onthedevelopmentofnovelinhibitorsforimprovingthetherapeuticwindowoffluoropyrimidinechemotherapy.BMCStructBiol.2009Mar16;9:14.[3].MonksA,et,al.Effectof5-benzylacyclouridine,apotentinhibitorofuridinephosphorylase,onthemetabolismofcirculatinguridinebytheisolatedratliver.BiochemPharmacol.1983Jul1;32(13):2003-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic