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当前位置: 首页 > 产品中心 > Small_molecule > Medchemexpress/盐酸异丙肾上腺素(同义词:盐酸异丙肾上腺素)/HY-B0468/10mM*1mL二甲基亚砜
商品详细Medchemexpress/盐酸异丙肾上腺素(同义词:盐酸异丙肾上腺素)/HY-B0468/10mM*1mL二甲基亚砜
Medchemexpress/盐酸异丙肾上腺素(同义词:盐酸异丙肾上腺素)/HY-B0468/10mM*1mL二甲基亚砜
Medchemexpress/盐酸异丙肾上腺素(同义词:盐酸异丙肾上腺素)/HY-B0468/10mM*1mL二甲基亚砜
商品编号: HY-B0468-10mM*1mLinDMSO
品牌: MedChemExp
市场价: ¥1060.00
美元价: 636.00
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
商品介绍
Isoprenaline(hydrochloride)isanon-selective beta-adrenergicreceptor agoNIST,usedforthetreatmentofbradycardiaandheartblock.
Description

Isoprenaline(hydrochloride)isanon-selective beta-adrenergicreceptor agonist,usedforthetreatmentofbradycardiaandheartblock.

InVitro

Isoprenaline(300nM,3min)increasesparticulatecGMP-andcilostamide-inhibited,low-KmcAMPphosphodiesterase(cAMP-PDE)activitybyabout100%inintactratfatcells[1]. Isoprenalineinhibitsinsulin-stimulatedglucosetransportactivityinratadipocytes.Isoprenaline,intheabsenceofadenosine,promotesatime-dependent(t1/2approximately2min)decreaseintheaccessibilityofinsulin-stimulatedcellsurfaceGLUT4of>50%,whichdirectlycorrelatedwiththeobservedinhibitionoftransportactivity[2]. Isoprenaline(5nMand10mM)increasescyclicAMPlevelsandthiseffectispotentiatedbycilostamide(10mM),byrolipram,acyclicAMP-specificPDE(PDE4)inhibitor(10mM)andbycyclicGMP-elevatingagents(50nMANFor30nMSNPplus100nMDMPPO)[3]. IsoprenalineincreasesthetranscriptionalactivityofGialpha-2geneto140%ofthecontrolvalue,whereasgenespecifichybridizationforGsalpharemainsunchanged[4]. Isoprenaline(20nM)increasestheamplitudeoftotaliKandcausesanegativeshiftofapproximately10mVintheactivationcurveforiK,bothintheabsenceandinthepresenceof300nMnisoldipinetoblocktheL-typeCa2+current.Isoprenaline(20nM)increasesthespontaneouspacemakerrateofsino-atrialnodepacemakercellsby16%inrabbitisolatedpacemakercells[5].

ClinicalTrial
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References
  • [1].DegermanE,etal.EvidencethatinsulinandisoprenalineactivatethecGMP-inhibitedlow-KmcAMPphosphodiesteraseinratfatcellsbyphosphorylation.ProcNatlAcadSciUSA.1990Jan;87(2):533-7.

    [2].VannucciSJ,etal.CellsurfaceaccessibilityofGLUT4glucosetransportersininsulin-stimulatedratADIposecells.Modulationbyisoprenalineandadenosine.BiochemJ.1992Nov15;288(Pt1):325-30.

    [3].DelpyE,etal.EffectsofcyclicGMPelevationonisoprenaline-inducedincreaseincyclicAMPandrelaxationinrataorticsmoothmuscle:roleofphosphodiesterase3.BrJPharmacol.1996Oct;119(3):471-8.

    [4].MullerFU,etal.IsoprenalinestimulatesgenetranscriptionoftheinhibitoryGproteinalpha-subunitGialpha-2inratheart.CircRes.1993Mar;72(3):696-700.

    [5].LeiM,etal.Modulationofdelayedrectifierpotassiumcurrent,iK,byisoprenalineinrabbitisolatedpacemakercells.ExpPhysiol.2000Jan;85(1):27-35.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM4.0368mL20.1841mL40.3682mL
5mM0.8074mL4.0368mL8.0736mL
10mM0.4037mL2.0184mL4.0368mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

Cellsareseededin24-wellculturedishesatadensityof2to5×104cellsperwell.Experimentsareperformedafter3to5daysinculturewhencellshasreachedconfluence.Culturemediumisaspiratedandreplacedby0.5mLofPBScontainingthepharmacologicalagents.Treatmentsareperformedinquadruplicateat37°C.Thetype3,4and5PDEinhibitorscilostamide(10gM),rolipram(10pM)andDMPPO(10gM),respectively,areincubatedwithcellsfor30minbeforeadditionofadenylateorguanylatecyclaseactivators.CyclicGMPandcyclicAMParerespectivelyincreasedinRASMCbystimulationofparticulateguanylatecyclasewithANF(50nMfor10min)orfl-adrenoceptorswithisoprenaline(5nmfor5min).Attheendoftheincubationperiod,themediumisremovedandintracellularcyclicnucleotidesareextractedbytwoethanolic(65%)ishesat4°Cfor5min.Ethanolicextractsarepooled,evaporatedtodrynessbyaSpeed-Vacsystem.Thedriedextractisdissolvedinasuitableamountofassaybufferandcyclicnucleotidelevelsaremeasuredbyscintillationproximityassay.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].DegermanE,etal.EvidencethatinsulinandisoprenalineactivatethecGMP-inhibitedlow-KmcAMPphosphodiesteraseinratfatcellsbyphosphorylation.ProcNatlAcadSciUSA.1990Jan;87(2):533-7.

    [2].VannucciSJ,etal.CellsurfaceaccessibilityofGLUT4glucosetransportersininsulin-stimulatedratadiposecells.Modulationbyisoprenalineandadenosine.BiochemJ.1992Nov15;288(Pt1):325-30.

    [3].DelpyE,etal.EffectsofcyclicGMPelevationonisoprenaline-inducedincreaseincyclicAMPandrelaxationinrataorticsmoothmuscle:roleofphosphodiesterase3.BrJPharmacol.1996Oct;119(3):471-8.

    [4].MullerFU,etal.IsoprenalinestimulatesgenetranscriptionoftheinhibitoryGproteinalpha-subunitGialpha-2inratheart.CircRes.1993Mar;72(3):696-700.

    [5].LeiM,etal.Modulationofdelayedrectifierpotassiumcurrent,iK,byisoprenalineinrabbitisolatedpacemakercells.ExpPhysiol.2000Jan;85(1):27-35.

MolecularWeight

247.72

Formula

C₁₁H₁₈ClNO₃

CASNo.

51-30-9

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:14.5mg/mL

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

Purity:99.97%