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商品详细Medchemexpress/SEA0400/HY-15515/10mg
Medchemexpress/SEA0400/HY-15515/10mg
Medchemexpress/SEA0400/HY-15515/10mg
商品编号： HY-15515-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥3520.00
美元价： 2112.00
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
SEA0400isanovelandselectiveinhibitoroftheNa+-Ca2+exchanger(NCX),inhibitingNa+-dependentCa2+uptakeinculturedneurons,astrocytes,andmicrogliawithIC50soffrom5to33nM.

CustomerValidation

  • •JClinInvest.2016Jan;126(1):112-22.
  • •JPhysiol.2015Aug1;593(15):3333-50.
  • •JPhysiol.2015Mar15;593(6):1459-77.
  • •JPhysiol.2014Nov15;592(Pt22):4969-93.
  • •CellSignal.2017May20;37:12-30.
  • •CellCalcium.2016Jul;60(1):25-31.
  • •AmJPhysiolHeartCircPhysiol.2016Dec1;311(6):H1352-H1359.
  • •PflugersArch.2015Oct;467(10):2151-63.
  • •BrainRes.2016Aug1;1644:249-57.
  • •BiochemBiophysRep.2017Mar;9:245-256.
  • •JACCBasicTranslSci.2016Jun;1(4):251-266.
Description

SEA0400isanovelandselectiveinhibitoroftheNa+-Ca2+exchanger(NCX),inhibitingNa+-dependentCa2+uptakeinculturedneurons,astrocytes,andmicrogliawithIC50soffrom5to33nM.

IC50&Target

IC50:5-33nM(NCX)

InVitro

SEA0400inhibitsNa+-dependent45Ca2+uptakeinculturedneurons,astrocytes,andmicroglia.IC50valuesofSEA0400are33nM(neurons),5.0nM(astrocytes),and8.3nM(microglia)[1].SEA0400preventssodiumnitroprusside(SNP)toincreaseERKandp38MAPKphosphorylation,andproductionofreactiveoxygenspecies(ROS)inanextracellularCa2+-dependentmanner[2].

InVivo

SEA0400(3mg/kg+3mg/kg/hfor2h,i.v.)attenuatestheinfarctvolumeinthecerebralcortexandstriatum,doesnotaffectthemeantheregionalcorticalbloodflowinanesthetizedrats[1].SEA0400protectsagainstthedopaminergicneurotoxicity(determinedbydopaminelevelsinthemidbrainandstriatum,tyrosinehydroxylaseimmunoreactivityinthesubstantianigraandstriatum,striataldopaminerelease,andmotordeficits)inMPTP-treatedC57BL/6Jmice[3].

References

  • [1].MatsudaT,etal.SEA0400,anovelandselectiveinhibitoroftheNa+-Ca2+exchanger,attenuatesreperfusioninjuryintheinvitroandinvivocerebralischemicmodels.JPharmacolExpTher.2001Jul;298(1):249-56.

    [2].NashidaT,etal.ThespecificNa(+)/Ca(2+)exchangeinhibitorSEA0400preventsnitricoxide-inducedcytotoxicityinSH-SY5Ycells.NeuRochemInt.2011Aug;59(1):51-8.

    [3].AgoY,etal.SEA0400,aspecificNa+/Ca2+exchangeinhibitor,preventsdopaminergicneurotoxicityinanMPTPmousemodelofParkinson"sdisease.Neuropharmacology.2011Dec;61(8):1441-51.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.6927mL13.4633mL26.9266mL
5mM0.5385mL2.6927mL5.3853mL
10mM0.2693mL1.3463mL2.6927mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

Na+-Ca2+exchangeactivityisdeterminedbyassayingNa+-dependent45Ca2+uptakeasreportedpreviously.Briefly,thecellsarepreincubatedinHanks"balancedsalinesolution(HBSS)for20min,andthemediumisswitchedtoHBSScontaining45Ca2+ andincubatedfor5min.ToincreaseintracellularNa+ concentration,1mMouabainplus20μMmonensin(forastrocytesandmicroglia)and10μMmonensin(forneurons)areused.Monensinisaddedsimultaneouslywiththeisotope.Ouabainisadded5minbeforemonensininastrocytesandmicroglia.SEA0400andKB-R7943areadded5minbeforemonensinandpresentduring45Ca2+ uptakereaction.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[1]

SEA0400isdissolvedinDMSO(finalconcentration0.1%).

Cells,platedin96-wellplastictissuecultureplates,areincubatedat37°Cfor30mininnormalorCa2+-freeHBSScontaining10μMH2DCF-DAand0.25μg/mLCremophorEL,andthenrinsedtwicewithnormalHBSStoremoveexcessdye.ThecellsarereperfusedinnormalHBSSfor1h,andtheconversionofH2DCF-DAtoitsfluorescentproductdichlorofluoresceinbyROS,presumablyH2O2andhydroxylrADIcal,isdeterminedwithexcitationat485nmandemissionat535nmusingaWallacMultilabelcounter.ROSproductionisexpressedasapercentageofcontrolcells.ThelinearityandsensitivityofROSassayareconfirmedusingH2O2priortotheexperiment.SEA0400attheindicatedconcentrationsisadded10minbeforeCa2+ reperfusionandpresentuntilassay. MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1]

SEA0400isadministratedasalipidemulsioncontaining20%soybeanoil.

MaleSprague-Dawleyrats,weighing289to325g,areanesthetizedwith1to2%halothane.Acatheterisinsertedintothefemoralarteryandconnectedtoapressuretransducertorecordbloodpressure.RegionalcorticalbloodflowismeasuredbyalaserDopplerflowmeter,withprobeplacementat2mmposteriorand6mmlateraltothebregma.SEA0400oritsvehiclewithanequivalentvolumeisi.v.injectedat3mg/kgandtheninfusedat3mg/kg/hfor2hundernormalconditionswithoutMCAocclusion.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].MatsudaT,etal.SEA0400,anovelandselectiveinhibitoroftheNa+-Ca2+exchanger,attenuatesreperfusioninjuryintheinvitroandinvivocerebralischemicmodels.JPharmacolExpTher.2001Jul;298(1):249-56.

    [2].NashidaT,etal.ThespecificNa(+)/Ca(2+)exchangeinhibitorSEA0400preventsnitricoxide-inducedcytotoxicityinSH-SY5Ycells.NeurochemInt.2011Aug;59(1):51-8.

    [3].AgoY,etal.SEA0400,aspecificNa+/Ca2+exchangeinhibitor,preventsdopaminergicneurotoxicityinanMPTPmousemodelofParkinson"sdisease.Neuropharmacology.2011Dec;61(8):1441-51.

MolecularWeight

371.38

Formula

C₂₁H₁₉F₂NO₃

CASNo.

223104-29-8

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥32mg/mL

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

Purity:99.89%