ASP-4058-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEASP-4058Cat.No.:HY-111021CASNo.:952565-91-2分⼦式:C₁₉H₁₂F₆N₄O₂分⼦量:442.31作⽤靶点:LPLReceptor作⽤通路:GPCR/GProtein储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:≥50mg/mL(113.04mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2609mL11.3043mL22.6086mL5mM0.4522mL2.2609mL4.5217mL10mM0.2261mL1.1304mL2.2609mL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(protectfromlight)。-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%salineSolubility:≥1.25mg/mL(2.83mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:1.25mg/mL(2.83mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(2.83mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ASP-4058⼀个选择性的、⼝服活性的鞘氨醇磷酸受体1和5(S1P1andS1P5)的⼆代激动剂，能改⼩⿏实验性⾃⾝免疫性脑脊髓炎，具有良好的安全性[1]。IC50&TargetS1P1andS1P5[1].体内研究ASP4058(p.o.,dailyfor21days)reducestheclinicalscoreinadose-dependentmannerandthecumulativeclinicalscorefromday0to21dpiat0.03,0.1and0.3mg/kgare15.5±1.48,9.50±2.17and1.17±1.17,respectively,whilethatofvehicle-treatedgroupis15.5±0.619inrats.ASP4058preventsdecreasesinbodyweightofEAErats[1].ASP4058(p.o.,dailyforday12today45)maintainstheclinicalscoreatarelativelylowlevelandthecumulativeclinicalscores(18-45dpi)amongthegroupstreatedwith0.1and0.3mg/kgdosagesare6.90±2.85and5.60±2.21,respectivelyinmice.TheED50valuesforASP4058is0.063mg/kg[1].AnimalModel:MaleLewisratswithaninductionofEAE[1].Dosage:0.03,0.1or0.3mg/kg.Administration:Oraladministrationoncedailyfor21days.Result:Reducedtheclinicalscoreinadose-dependentmannerandthecumulativeclinicalscore.AnimalModel:SJLmiceimmunizedwithPLP139-151andboostedwithpertussistoxindevelopedrelapsing-remittingEAE[1].Dosage:0.1and0.3mg/kgAdministration:Oraladministrationoncedailyfromday12today45.Result:Maintainedtheclinicalscoreatarelativelylowlevelandthecumulativeclinicalscores(18-45dpi).户使⽤本产品发表的科研⽂献•SciAdv.2020May29;6(22):eaay8627.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].RieYamamoto,etal.ASP4058,aNovelAgonistforSphingosine1-PhosphateReceptors1and5,AmelioratesRodentExperimentalAutoimmuneEncephalomyelitiswithaFavorableSafetyProfile.PLoSOne.2014Oct27;9(10):e110819.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo