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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Bay 60-7550(Synonyms: BAY 607550)/HY-14992/100mg
商品详细Medchemexpress/Bay 60-7550(Synonyms: BAY 607550)/HY-14992/100mg
Medchemexpress/Bay 60-7550(Synonyms: BAY 607550)/HY-14992/100mg
Medchemexpress/Bay 60-7550(Synonyms: BAY 607550)/HY-14992/100mg
商品编号： HY-14992-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥5800.00
美元价： 3480.00
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
Bay60-7550isaselectiveinhibitorofPDE2withKiof3.8±0.2nM,alsoisamodulatorofNO.
Description

Bay60-7550isaselectiveinhibitorofPDE2withKiof3.8±0.2nM,alsoisamodulatorofNO.

IC50&Target

Ki:3.8±0.2nM(PDE2)[1]

InVitro

Bay60-7550(1μM)increasescGMPintheneuronalculturescomparedwithcontrol[F(6,14)=12.97,p<0.05 for="" bay="" 60-7550].="" bay="" 60-7550="" in="" the="" presence="" of="" nmda="" (30="" μm)="" results="" in="" further="" increases="" in="" cgmp="" compared="" with="" nmda="" alone.="" the="" nmda="" receptor="" antagonist="" mk-801="" (10="" μm)="" blocks="" both="" bay="" 60-7550+nmda-induced="" elevation="" in="" cgmp="" in="" neuronal="">[1].Comparedwithuntreatedcontrolcells,proliferationofPASMCsfromIPAHpatientsissignificantlyreducedbyBAY60-7550(1μM)[2].

InVivo

ThePDE2inhibitorsBay60-7550(1mg/kg)reversesrestraintstress-inducedalterationsinbehavior,resultinginincreasedpercentagesofopen-armentriesandopen-armtimecomparedwiththevehicle+restraintstresscondition.Innonstressedmice,Bay60-7550producesadose-dependentincreaseinpercentagesofopen-armentriesandopen-armtimecomparedwiththevehicle-treatedgroup;significantincreasesareobservedatadoseof3mg/kg.Innonstressedmice,Bay60-7550increases,inadose-dependentmanner,thenumberofhead-dipsandtimespenthead-dipping,comparedwithvehicle-treatedmice;significantincreasesareobservedatdosesof1and3mg/kg[1].

References

  • [1].MasoodA,etal.Anxiolyticeffectsofphosphodiesterase-2inhibitorsassociatedwithincreasedcGMPsignaling.JPharmacolExpTher.2009Nov;331(2):690-9.

    [2].BubbKJ,etal.Inhibitionofphosphodiesterase2augmentscGMPandcAMPsignalingtoamelioratepulmonaryhypertension.Circulation.2014Aug5;130(6):496-507.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.0983mL10.4916mL20.9833mL
5mM0.4197mL2.0983mL4.1967mL
10mM0.2098mL1.0492mL2.0983mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

COS-7cellsaremaintainedincompleteDMEM(containing10%fetalcalfserum,100units/mLpenicillinG,100mg/mLstreptomycin,and400μML-alanyl-L-glutamine)at37°Cin5%CO2atmosphere.APDE2expressionplasmidisintroducedintoCOS-7cellsusingtheFuGENE6transfectionreagent.Cellsarelysedinsolubilizationbuffer(275mMNaCl,1.5mMMgCl2,2mMEGTA,2%TritonX,20%glycerol,and40mMTris-HCl),andthecelllysatesareusedintheimmunoprecipitationprocedures.AproteinA-agarosebeadslurry(100μL)iswashedthreetimeswithice-coldphosphate-bufferedsaline(100mMNaCl,2.7mMKCl,10.6mMNa2HPO4,and1.6mMNaH2PO4)andmixedwiththe5μgofPDE2antibodyand100μL(2μg/μL)ofthelysatesampleandrotatedovernightat4°C.Thebead/samplemixtureisthencentrifugedat1000gtoseparatethebeadsfromthesupernatant.ThebeadsareresUSPendedin100μLofice-coldlysisbuffer(20mMTris,pH7.4,140mMNaCl,0.75mMMgCl2,1mMEGTA,1%TritonX-100,and20%glycerol,containingproteaseandphosphataseinhibitors)toelutethePDE2foruseintheenzymeactivityassays.ThePDE2activityassayisdone.TherecombinantPDE2enzymederivedfromCOS-7cellexpressionanddilutedinKHEMbuffer(50mMKCl,50mMHEPES,10mMEGTA,and1.9mMMgCl2,pH7.2)ismixedwithdifferentconcentrationsofPDE2inhibitors(Bay60-7550,ND7001,andEHNA)and[3H]cGMP/cGMP(5μM)asthesubstrate.Themixtureisthenincubatedfor30minat37°C(100μLofreactionvolume).Toconvertthe[3H]GMPto[3H]guanosine,samplesareincubatedwithsnakevenomfromCrotalusatroxfor30minat37°C.ThesamplesarethenvortexedwithafreshlypreparedslurryofDowex/water/ethanol[1:1:1,v/v]andthencentrifugedfor10min.[3H]Guanosineinthesupernatantisthenquantifiedbyliquidscintillationcounting.Bay60-7550isdissolvedindimethylsulfoxide,EHNAisdissolvedindistilledwater,andND7001isdissolvedinethanolas10mMstocksandthendilutedforuseinassayswith20mMTris,pH7.4;finalconcentrationsoftherespectivesolventsdidnotaffecttheassay.IC50valuesatasinglesubstrateconcentrationaredeterminedbynonlinearregressionanalysisofthelogconcentration-responsecurvesforeachPDE2inhibitor;Kivaluesarecalculated[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[2]

Bay60-7550isdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[1].

Growthofhumandistalpulmonaryarterysmoothmusclecellsisolatedfrompatientswithidiopathicpulmonaryarterialhypertension(IPAH)orcontrolcellsfromadultsundergoingtransplantorlungresectionforsuspectedmalignancy,aremonitoredfollowingtreatmentwithBAY60-7550(1μM),ANP(1μM),DETA-NONOate(10μM),orTreprostinil(1μM),aloneorincombination[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1]

Bay60-7550isdissolvedin50%DMSOanddilutedwithsalineorPBS[1].

Mice[1]
MaleICRmiceweighing28to35gareused.Bay60-7550(0.5,1,and3mg/kg),ND7001(0.5,1.0,and3mg/kg),Detanonoate(0.5mg/kg),L-NAME(50mg/kg),orDiazepam(1mg/kg)isadministeredafterrestraintstressand30minbeforebehavioraltesting.MicealsoaretreatedwithBay60-7550(3mg/kg),ND7001(3mg/kg),Detanonoate,(0.5mg/kg),L-NAME(50mg/kg),ordiazepam(1mg/kg)intheabsenceofrestraintstress;drugsareadministered30minbeforethebehavioraltests.Bay60-7550shows50-foldselectivityforPDE2comparedwithPDE1,100-foldcomparedwithPDE5,andgreaterthan200-foldcomparedwiththeotherPDEfamilies.ND7001exhibitsat1east100-foldselectivityforinhibitionofPDE2relativetootherPDEfamilies.ForantagonismteststoassesstheroleofcGMPsignalinginthebehavioraleffectsofthePDE2inhibitors,ODQ,aninhibitorofsolubleguanylylcyclase(20mg/kg),isadministered20minbeforeBay60-7550orND7001.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].MasoodA,etal.Anxiolyticeffectsofphosphodiesterase-2inhibitorsassociatedwithincreasedcGMPsignaling.JPharmacolExpTher.2009Nov;331(2):690-9.

    [2].BubbKJ,etal.Inhibitionofphosphodiesterase2augmentscGMPandcAMPsignalingtoamelioratepulmonaryhypertension.Circulation.2014Aug5;130(6):496-507.

MolecularWeight

476.57

Formula

C₂₇H₃₂N₄O₄

CASNo.

439083-90-6

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:98.12%