SRT-1720-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESRT1720Cat.No.:HY-10532CASNo.:925434-55-5分⼦式:C₂₅H₂₃N₇OS分⼦量:469.56作⽤靶点:Sirtuin;Autophagy作⽤通路:CellCycle/DNADamage;Epigenetics;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(133.10mM;ultrasonicandadjustpHto5withHCl)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1297mL10.6483mL21.2965mL5mM0.4259mL2.1297mL4.2593mL10mM0.2130mL1.0648mL2.1297mL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%salineSolubility:≥2.08mg/mL(4.43mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.43mM);Clearsolution3.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:25mg/mL(53.24mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性SRT1720⼈SIRT1的有效激活剂，EC1.5值为0.16μM，对SIRT2和SIRT3的作⽤较弱，EC1.5值分别为37μM和>300μM。IC50&TargetSIRT1SIRT20.16μM(EC1.5)37μM(EC1.5)体外研究SRT1720effectivelydecreasestheacetylationofp53incellsevenintheabsenceofSIRT1,andthisisattributedtoinhibitionofhistoneacetyltransferasep300[2].体内研究SRT1720(10,30,100mg/kg,p.o.)significantlyreducesthehyperinsulinaemiaafter4weeks,partiallynormalizingelevatedinsulinlevelssimilartorosiglitazonetreatment.SRT1720treatmentsignificantlyreducesfastingbloodglucosetonearnormallevelsinLepob/obmice[1].SRT1720hasabilitytoprotectagainstthenegativeeffectsofdiet-inducedobesityinmice,andhasaconnectiontometabolicadaptationinfattyacidandoxidativemetabolismthroughdownstreamtargetsofSIRT1suchasPGC1αandFOXO1[2].SRT1720(50-100mg/kg,p.o.),duringemphysemadevelopmentattenuateselastase-inducedairspaceenlargementandlungfunctionimpairmentaswellasreducesarterialoxygensaturationinWTmice[3].PROTOCOLAnimalMice:NineweekoldC57BL/6malemicearefedahighfatdiet(60%caloriesfromfat)untiltheirmeanbodyAdministration[1]weightreachapproximately40g.Themicearethendividedintotestgroups(6-10pergroup).SRT1460(100mg/kg),SRT1720(100mg/kg),SRT501(500mg/kg)androsiglitazone(5mg/kg)areadministeredoncedailyviaoralgavage.Thevehicleusedis2%HPMC+0.2%DOSS.Individualmousebodyweightsaremeasuredtwiceweekly.At2,4,6,8and10weeksofdosingafedbloodglucosemeasureistakenandafter5weeksoftreatmentanIPGTTisconductedonallmicefromeachofthegroups.After10weeksoftreatment,anITTisconducted.StatisticalanalysisiscompletedusingtheJMPprogram.DataareanalyzedbyaonewayANOVAwithcomparisontocontrolusingaDunnett’sTest.Apvalue<0.05indicatesasignificantdifferencebetweengroups.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellMolImmunol.2022Jun23;1-11.•SciAdv.2022Apr8;8(14):eabj7110.•ActaPharmSinB.27August2022.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•ProcNatlAcadSciUSA.2019Feb19;116(8):2961-2966.•AgingCell.2021Oct3;e13491.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MilneJCetal.SmallmoleculeactivatorsofSIRT1astherapeuticsforthetreatmentoftype2diabetes.Nature.2007Nov29;450(7170):712-6[2].BaurJA,etal.Aresirtuinsviabletargetsforimprovinghealthspanandlifespan?NatRevDrugDiscov.2012Jun1;11(6):443-61[3].YaoH,etal.SIRT1protectsagainstemphysemaviaFOXO3-mediatedreductionofprematuresenescenceinmice.JClinInvest.2012Jun1;122(6):2032-45.[4].YuL,etal.ProtectiveeffectsofSRT1720viatheHNF1α/FXRsignallingpathwayandanti-inflammatorymechanismsinmicewithestrogen-inducedcholestaticliverinjury.ToxicolLett.2016Dec15;264:1-1