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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/罗格列酮（同义词：BRL49653）/HY-17386/50mg
商品详细Medchemexpress/罗格列酮（同义词：BRL49653）/HY-17386/50mg
Medchemexpress/罗格列酮（同义词：BRL49653）/HY-17386/50mg
Medchemexpress/罗格列酮（同义词：BRL49653）/HY-17386/50mg
商品编号： HY-17386-10mM*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
电话号码： 4000-520-616
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商品介绍
Rosiglitazoneisaperoxisomeproliferator-activatedreceptor-gamma(PPAR-γ)agoNIST,andisablockerofTRPM2andTRPM3channels.

CustomerValidation

  • •FrontMolNeurosci.2017Sep14;10:293.
  • •ChinesePharmacologicalBulletin.2017,33(4):517-521.
Description

Rosiglitazoneisaperoxisomeproliferator-activatedreceptor-gamma(PPAR-γ)agonist,andisablockerofTRPM2andTRPM3channels.

IC50&Target

TRPM2andTRPM3blocker[1]
PPARagonist[2]

InVitro

TRPM2isunaffectedbyRosiglitazoneatconcentrationsupto10μMbutisinhibitedcompletelyathigherconcentrations(IC50~22.5μM).TRPC5isstronglystimulatedbyRosiglitazoneatconcentrationsof10μMandgreater(EC50~30μM).LowconcentrationsofRosiglitazone(0.1-1μM)causeabout20%inhibitionofTRPM3.HigherconcentrationsofRosiglitazonecausestrongerandcompleteTRPM3inhibitionwithIC50valuesof9.5μMand4.6μMagainstnifedipine-andPregS-evokedactivity[1].Rosiglitazoneisaperoxisomeproliferator-activatedreceptor-γ(PPARγ)agonist,whichisananti-diabeticagentagainsttype2diabetes[2].

InVivo

RosiglitazonepreventsEndotoxinlethalitybyattenuatingHMGB1release.BALB/cmice(n=10-11pergroup)areinjectedwithasingledoseofRosiglitazone(10mg/kg,i.p.)withorwithoutGW9662(1mg/kg,i.p.),followed30minlaterbyalethalinfusionofEndotoxin(LPS,10mg/kg,i.p.)[3].

ClinicalTrial
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References

  • [1].MajeedY,etal.RapidandcontrastingeffectsofRosiglitazoneontransientreceptorpotentialTRPM3andTRPC5channels.MolPharmacol.2011Jun;79(6):1023-30.

    [2].YoonSY,etal.RosiglitazonereducestauphosphorylationviaJNKinhibitioninthehippocampusofratswithtype2diabetesandtautransfectedSH-SY5Ycells.NeurobiolDis.2010Nov;40(2):449-55.

    [3].HwangJS,etal.ActivationofPeroxisomeProliferator-ActivatedReceptorγbyRosiglitazoneInhibitsLipopolysaccharide-InducedReleaseofHighMobilityGroupBox1.MediatorsInflamm.2012;2012:352807.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.7978mL13.9888mL27.9775mL
5mM0.5596mL2.7978mL5.5955mL
10mM0.2798mL1.3989mL2.7978mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

RosiglitazoneisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[2].

HumanneuroblastomaSH-SY5YcellsaremaintainedinDulbecco"smodifiedEagle"smedium(DMEM)supplementedwith10%fetalbovineserum,100μg/mLStreptomycinand100U/mLPenicillinG.SH-SY5Ycellsaretransfectedwiththelongestisoformofhumantau(2N4R)taggedwithGFPusinglipofectamine.24hraftertransfection,cellsaretreatedwithRosiglitazone(10μM,50μM)for24hr[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2][3]

RosiglitazoneispreparedinDMSO,andthendilutedin0.5%carboxymethylcelluloseindrinkingwatertomaximizesolubility.

Rats[2]
OLETFratsaredividedrandomlyintotwogroups(n=6or7animalspergroup)at21weeksofage.Ratsaregivenstandardratfoodorratfoodsupplementedwith3mg/kg/dayRosiglitazonefor27weeks.UrinaryglucoseismonitoredweeklyusingDiastix.Individualratsarediagnosedasdiabeticwhenpositiveglycosuriaisidentified.C57BL6micearedividedrandomlyintotwogroups(n=7animalspergroup)at10weeksofage.Micereceivedasingleintraperitonealinjectionof150mg/kgofSTZin0.5Msodiumcitratebufferand,after3days,3mg/kgofRosiglitazoneorvehiclearedailyadministeredperosfor4consecutivedays.Micewithglycemiaover11mMglucosearediagnosedasdiabetic.
Mice[3]
BALB/cmicearerandomlyassignedtooneoffourgroups:injectionofLPS(10mg/kg),injectionofLPS(10mg/kg)plusRosiglitazone(10mg/kg),injectionofLPS(10mg/kg)plusRosiglitazone(10mg/kg)plusGW9662(1mg/kg),orinjectionofGW9662(1mg/kg)alone.AnothergroupofBALB/cmicearetreatedwithRosiglitazone(10mg/mL)afterLPS(10mg/kg)infusion.Mortalityisrecordedforupto2weeksafterLPSinjectiontoensurethatnoadditionallatedeathsoccurred.FormeasurementofplasmaHMGB1levels,BALB/cmicearesubjectedtosepsisbyLPSinjectioninthepresenceorabsenceofRosiglitazone.After20h,bloodiscollected,allowedtoclotfor2hatroomtemperature,andthencentrifugedfor20minat1,500g.ThelevelsofcirculatingHMGB1inserumaredeterminedbyWesternblotanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].MajeedY,etal.RapidandcontrastingeffectsofRosiglitazoneontransientreceptorpotentialTRPM3andTRPC5channels.MolPharmacol.2011Jun;79(6):1023-30.

    [2].YoonSY,etal.RosiglitazonereducestauphosphorylationviaJNKinhibitioninthehippocampusofratswithtype2diabetesandtautransfectedSH-SY5Ycells.NeurobiolDis.2010Nov;40(2):449-55.

    [3].HwangJS,etal.ActivationofPeroxisomeProliferator-ActivatedReceptorγbyRosiglitazoneInhibitsLipopolysaccharide-InducedReleaseofHighMobilityGroupBox1.MediatorsInflamm.2012;2012:352807.

MolecularWeight

357.43

Formula

C₁₈H₁₉N₃O₃S

CASNo.

122320-73-4

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥180mg/mL

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

Purity:99.46%