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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/GW 501516（同义词：GW 1516；GSK-516）/HY-10838/10mM*1mL二甲基亚砜
商品详细Medchemexpress/GW 501516（同义词：GW 1516；GSK-516）/HY-10838/10mM*1mL二甲基亚砜
Medchemexpress/GW 501516（同义词：GW 1516；GSK-516）/HY-10838/10mM*1mL二甲基亚砜
Medchemexpress/GW 501516（同义词：GW 1516；GSK-516）/HY-10838/10mM*1mL二甲基亚砜
商品编号： HY-10838-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
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
GW501516isaPPARδagoNISTwithanEC50of1.1nM.
Description

GW501516isaPPARδagonistwithanEC50of1.1nM.

IC50&Target

EC50:1.1nM(PPARδ)[1]

InVitro

GW501516isshowntobethemostpotentandselectivePPARαagonistsknownwithanEC50of1.1nMagainstPPARαand1000-foldselectivityovertheotherhumansubtypes,PPARαand-γ[1].GW501516exertsanti-inflammatoryeffectsinmouseculturedproximaltubular(mProx)cells.GW501516inhibitspalmitate-andTNFα-inducedincreasesinMCP-1mRNAexpressioninadose-dependentmanner[3].

InVivo

GW501516causesimpairedboneformation,leADIngtodecreasedBMDanddeteriorationofbonepropertiesinOVXrats[2].GW501516attenuatesinterstitialinflammationandproximaltubularcelldamageinaprotein-overloadmousenephropathymodel[3].GW501516treatmentenhancesrunningenduranceandtheproportionofsuccinatedehydrogenase(SDH)-positivemusclefibresinbothtrainedanduntrainedmice[4].

References

  • [1].WeiZL,etal.AshortandefficientsynthesisofthepharmacologicalresearchtoolGW501516fortheperoxisomeproliferator-activatedreceptordelta.JOrgChem.2003Nov14;68(23):9116-8.

    [2].MostiMP,etal.Effectsoftheperoxisomeproliferator-activatedreceptor(PPAR)-δagonistGW501516onboneandmuscleinovariectomizedrats.Endocrinology.2014Jun;155(6):2178-89.

    [3].YangX,etal.GW501516,aPPARδagonist,amelioratestubulointerstitialinflammationinproteinurickidneydiseaseviainhibitionofTAK1-NFκBpathwayinmice.PLoSOne.2011;6(9):e25271.

    [4].ChenW,etal.AmetabolomicstudyofthePPARδagonistGW501516forenhancingrunningenduranceinKunmingmice.SciRep.2015May6;5:9884.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.2051mL11.0254mL22.0507mL
5mM0.4410mL2.2051mL4.4101mL
10mM0.2205mL1.1025mL2.2051mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

GW501516isdissolvedinDMSO.Cellsarestarvedbyincubationin0.2%FCSDMEMfor9h,thenpre-incubatedwithGW501516,atafinalconcentrationof2.5and5µM,or0.05%DMSOascontrolfor3hours,followedbystimulationwith150µMpalmitateboundto8.0%BSAfor12h[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2][3]

Rat:FemaleSpragueDawleyrats,12weeksofage,areallocatedtoasham-operatedgroupand3OVXgroups;high-doseGW501516(OVX-GW5),low-doseGW501516(OVX-GW1),andacontrolgroup(OVX-CTR),respectively.AnimalsreceiveGW501516orvehicle(methylcellulose)dailyfor4monthsbygavage.Bonemineraldensity(BMD)isassessedbydualx-rayabsorptiometryatthefemur,spine,andwholebody[2].

Mouse:Micearerandomlyallocatedtodifferentgroupsandreceivetherapeuticdietandtreatment.TheGW501516-containingrodentdietismadebyevenlyaddingGW501516tothecontroldiettoafinalconcentrationof0.04%w/w.Inthecontroldiet,10%ofthetotalcaloriesarefromfat(5.5%fromsoybeanoiland4.5%fromlard)[3].

MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].WeiZL,etal.AshortandefficientsynthesisofthepharmacologicalresearchtoolGW501516fortheperoxisomeproliferator-activatedreceptordelta.JOrgChem.2003Nov14;68(23):9116-8.

    [2].MostiMP,etal.Effectsoftheperoxisomeproliferator-activatedreceptor(PPAR)-δagonistGW501516onboneandmuscleinovariectomizedrats.Endocrinology.2014Jun;155(6):2178-89.

    [3].YangX,etal.GW501516,aPPARδagonist,amelioratestubulointerstitialinflammationinproteinurickidneydiseaseviainhibitionofTAK1-NFκBpathwayinmice.PLoSOne.2011;6(9):e25271.

    [4].ChenW,etal.AmetabolomicstudyofthePPARδagonistGW501516forenhancingrunningenduranceinKunmingmice.SciRep.2015May6;5:9884.

MolecularWeight

453.5

Formula

C₂₁H₁₈F₃NO₃S₂

CASNo.

317318-70-0

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.26%