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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/ST 2825/HY-50937/1mg
商品详细Medchemexpress/ST 2825/HY-50937/1mg
Medchemexpress/ST 2825/HY-50937/1mg
Medchemexpress/ST 2825/HY-50937/1mg
商品编号： HY-50937-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥38100.00
美元价： 22860.00
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
电子邮箱： info@ebiomall.com
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商品介绍
ST2825isaMyD88homodimerizationinhibitor.

CustomerValidation

  • •Gut.2017Sep12.pii:gutjnl-2017-314098.
  • •ACSNano.2015Oct27;9(10):10498-515.
  • •BrJPharmacol.2015Jun;172(12):3159-76.
  • •ExpNeurol.2017May18;295:23-35.
  • •SciRep.2017Nov17;7(1):15797.
  • •SciRep.2017Mar17;7:44822.
  • •PLoSOne.2014Jul18;9(7):e100985.
  • •BrainRes.2016Jul15;1643:130-9.
  • •AnticancerRes.2017Nov;37(11):6203-6209.
  • •MolMedRep.2015Jul;12(1):895-904.
  • •GenetMolRes.2016Mar4;15(1):15016826.
Description

ST2825isaMyD88homodimerizationinhibitor.

IC50&Target

MyD88[1]

InVitro

ST2825blocksIL-1R/TLRsignalingbyinterferingwithMyD88homodimerization.ST2825inhibitsthisinteractioninaconcentration-dependentmannerwith~40%inhibitionofdimerizationat5μMST2825and80%inhibitionat10μMST2825[1].

InVivo

ST2825dose-dependentlyinhibitsIL-1β-inducedproductionofIL-6intreatedmiceafteroraladmiNISTration.TheanimalsareadministeredorallywiththeappropriatevehiclesorST2825atdosesrangingfrom50to200mg/kg,5minpriortoi.p.injectionwith20μg/kgIL-1β.ST2825exertesasignificantinhibitionofIL-1β-stimulatedproductionofIL-6at100and200mg/kg[1].

References

  • [1].LoiarroM,etal.Pivotaladvance:inhibitionofMyD88dimerizationandrecruitmentofIRAK1andIRAK4byanovelpeptidomimeticcompound.JLeukocBiol.2007Oct;82(4):801-10.

    [2].FantòN,etal.Design,Synthesis,andInVitroActivityofPeptidomimeticInhibitorsofMyeloidDifferentiationFactor88.JMedChem.2008Mar13;51(5):1189-202.

    [3].VanTassellBW,etal.PharmacologicInhibitionofMyeloidDifferentiationFactor88(MyD88)PreventsLeftVentricularDilationandHypertrophyAfterExperimentalAcuteMyocardialInfarctionintheMouse.JCardiovascPharmacol.2010Apr;55(4):385-90.

    [4].ZhangHS,etal.Inhibitionofmyeloiddifferentiationfactor88(MyD88)byST2825providesneuroprotectionafterexperimentaltraumaticbraininjuryinmice.BrainRes.2016Jul15;1643:130-9.

    [5].WangN,etal.Myeloiddifferentiationfactor88isup-regulatedinepilepticbrainandcontributestoexperimentalseizuresinrats.ExpNeurol.2017Sep;295:23-35.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.6906mL8.4529mL16.9059mL
5mM0.3381mL1.6906mL3.3812mL
10mM0.1691mL0.8453mL1.6906mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

ST2825isdissolvedinDMSOandstored,andthendilutedwithappropriatemedia(DMSO0.1%)beforeuse[1].

HeLacellsareseededat105cells/mLina96-welltissue-cultureplate.Afterincubatingovernight,themediumisdiscarded,andthecellsareaddedwithtissueculturemedium,10%FBS,containingST2825atconcentrationsrangingfrom0.1to10μMandDMSOat0.1%finalconcentration.Thecellsareincubatedfor6and18handthenaddedwiththeyellowXTT(0.3mg/mL)forfurther2hofincubation.Attheendoftheincubationperiods,reactionsarequantifiedbyusingaSirioSSeacmicroplatereader[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1]

ST2825isadministeredorallyas0.5%sUSPensionincarboxymethylcellulose(CMC)[1].

Mice[1]
Mice(femaleC57Bl/6)aredividedintoexperimentalgroupsof15mice.Theyareinjectedi.p.withsaline(controlanimals)orrecombinantmurineIL-1β(20μg/kg).Atime-courseanalysisofIL-6productionestablishedthatthepeakofcytokineisreached2hafterIL-1βinjection.ST2825,administeredorallyas0.5%suspensionincarboxymethylcellulose(CMC)orCMCalone,issuppliedtotheexperimentalmicegroups.TwohoursafterIL-1βinjection,theanimalsarekilled,andseraarecollectedtoassayIL-6levels.Mice,whicharetreatedorallywith100and200mg/kgST2825,showslowerlevelsofIL-6versusCMC-treatedmice.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].LoiarroM,etal.Pivotaladvance:inhibitionofMyD88dimerizationandrecruitmentofIRAK1andIRAK4byanovelpeptidomimeticcompound.JLeukocBiol.2007Oct;82(4):801-10.

    [2].FantòN,etal.Design,Synthesis,andInVitroActivityofPeptidomimeticInhibitorsofMyeloidDifferentiationFactor88.JMedChem.2008Mar13;51(5):1189-202.

    [3].VanTassellBW,etal.PharmacologicInhibitionofMyeloidDifferentiationFactor88(MyD88)PreventsLeftVentricularDilationandHypertrophyAfterExperimentalAcuteMyocardialInfarctionintheMouse.JCardiovascPharmacol.2010Apr;55(4):385-90.

    [4].ZhangHS,etal.Inhibitionofmyeloiddifferentiationfactor88(MyD88)byST2825providesneuroprotectionafterexperimentaltraumaticbraininjuryinmice.BrainRes.2016Jul15;1643:130-9.

    [5].WangN,etal.Myeloiddifferentiationfactor88isup-regulatedinepilepticbrainandcontributestoexperimentalseizuresinrats.ExpNeurol.2017Sep;295:23-35.

MolecularWeight

591.51

Formula

C₂₇H₂₈Cl₂N₄O₅S

CASNo.

894787-30-5

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

ST2825isdissolvedinDMSO.ST2825solution(0.5μL)isadministeredviaintracerebroventricular(ICV)injectionat15minpost-injury,usinga1μLHamiltonmicrosyringe[4].
ST2825isdissolvedin10%dimethylsulfoxidein0.1MPBS[5].

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

References

  • [1].LoiarroM,etal.Pivotaladvance:inhibitionofMyD88dimerizationandrecruitmentofIRAK1andIRAK4byanovelpeptidomimeticcompound.JLeukocBiol.2007Oct;82(4):801-10.

    [2].FantòN,etal.Design,Synthesis,andInVitroActivityofPeptidomimeticInhibitorsofMyeloidDifferentiationFactor88.JMedChem.2008Mar13;51(5):1189-202.

    [3].VanTassellBW,etal.PharmacologicInhibitionofMyeloidDifferentiationFactor88(MyD88)PreventsLeftVentricularDilationandHypertrophyAfterExperimentalAcuteMyocardialInfarctionintheMouse.JCardiovascPharmacol.2010Apr;55(4):385-90.

    [4].ZhangHS,etal.Inhibitionofmyeloiddifferentiationfactor88(MyD88)byST2825providesneuroprotectionafterexperimentaltraumaticbraininjuryinmice.BrainRes.2016Jul15;1643:130-9.

    [5].WangN,etal.Myeloiddifferentiationfactor88isup-regulatedinepilepticbrainandcontributestoexperimentalseizuresinrats.ExpNeurol.2017Sep;295:23-35.

Purity:99.51%