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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/SRT 1720 Hydrochloride(Synonyms: SRT1720)/HY-15145/10mM*1mL in DMSO
商品详细Medchemexpress/SRT 1720 Hydrochloride(Synonyms: SRT1720)/HY-15145/10mM*1mL in DMSO
Medchemexpress/SRT 1720 Hydrochloride(Synonyms: SRT1720)/HY-15145/10mM*1mL in DMSO
Medchemexpress/SRT 1720 Hydrochloride(Synonyms: SRT1720)/HY-15145/10mM*1mL in DMSO
商品编号： HY-15145-5mg
品牌： MedChemExp
市场价： ¥2640.00
美元价： 1584.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
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商品介绍
SRT1720HydrochlorideisaselectiveactivatorofhumanSIRT1withanEC1.5of0.16μM,andshowslesspotentactivitiesagaiinstSIRT2andSIRT3withEC1.5sof37μMand>300μM,respectively.

CustomerValidation

  • •Hypertension.2016Nov;68(5):1191-1199.
Description

SRT1720HydrochlorideisaselectiveactivatorofhumanSIRT1withanEC1.5of0.16μM,andshowslesspotentactivitiesagaiinstSIRT2andSIRT3withEC1.5sof37μMand>300μM,respectively.

IC50&Target

EC1.5:0.16μM(SIRT1),37μM(SIRT2),>300μM(SIRT3)[1]

InVitro

SRT1720andSRT2183areabletoeffectivelydecreasetheacetylationofp53incellsevenintheabsenceofSIRT1,andthisisattributedtoinhibitionofhistoneacetyltransferasep300[2].

InVivo

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].

References

  • [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.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.9762mL9.8810mL19.7621mL
5mM0.3952mL1.9762mL3.9524mL
10mM0.1976mL0.9881mL1.9762mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdmiNISTration
[1]

SRT1720isformulatedin2%HPMC+0.2%DOSS.

NineweekoldC57BL/6malemicearefedahighfatdiet(60%caloriesfromfat)untiltheirmeanbodyweightreachapproximately40g.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<0.05=""indicates=""a=""significant=""difference=""between=""groups.=""mce=""has=""not=""independently=""confirmed=""the=""accuracy=""of=""these=""methods.=""they=""are=""for=""reference="">

References

  • [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.

MolecularWeight

506.02

Formula

C₂₅H₂₄ClN₇OS

CASNo.

1001645-58-4

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

SRT1720ispreparedinvehicle(normalsaline)[4].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References

  • [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.

Purity:98.79%