SRT-1720-dihydrochloride-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESRT1720dihydrochlorideCat.No.:HY-15145ACASNo.:2468639-77-0分⼦式:C₂₅H₂₅Cl₂N₇OS分⼦量:542.48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:85mg/mL(156.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8434mL9.2169mL18.4339mL5mM0.3687mL1.8434mL3.6868mL10mM0.1843mL0.9217mL1.8434mL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。BIOLOGICALACTIVITY⽣物活性SRT1720dihydrochloride选择性的和具有⼝服活性的SIRT1激活剂，EC50为0.10μM，对SIRT2和SIRT3的作⽤较弱。IC50&TargetSIRT10.10μM(EC50)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究SRT1720dihydrochlorideeffectivelydecreasestheacetylationofp53incellsevenintheabsenceofSIRT1,andthisisattributedtoinhibitionofhistoneacetyltransferasep300[2].体内研究SRT1720(10,30,100mg/kg,p.o.)dihydrochloridetreatmentsignificantlyreducesfastingbloodglucosetonearnormallevelsinLepob/obmice[1].SRT1720dihydrochloridehasabilitytoprotectagainstthenegativeeffectsofdiet-inducedobesityinmice,andhasaconnectiontometabolicadaptationinfattyacidandoxidativemetabolismthroughdownstreamtargetsofSIRT1suchasPGC1αandFOXO1[2].SRT1720(50-100mg/kg,p.o.)dihydrochloride,duringemphysemadevelopmentattenuateselastase-inducedairspaceenlargementandlungfunctionimpairmentaswellasreducesarterialoxygensaturationinWTmice[3].PROTOCOLAnimalMice:NineweekoldC57BL/6malemicearefedahighfatdiet(60%caloriesfromfat)untiltheirmeanbodyAdministration[1]weightreachapproximately40g.Themicearethendividedintotestgroups(6-10pergroup).SRT1460(100mg/kg),SRT1720(100mg/kg),SRT501(500mg/kg)andBRL49653(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.•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].GaoD,etal.ActivationofSIRT1AttenuatesKlothoDeficiency-InducedArterialStiffnessandHypertensionbyEnhancingAMP-ActivatedProteinKinaseActivity.Hypertension.2016Nov;68(5):1191-1199.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[5].LahusenTJ,etal.SRT1720induceslysosomal-dependentcelldeathofbreastcancercells.MolCancerTher.2015Jan;14(1):183-92.McePdfHeightCaution:Pr