Levcromakalim-minus-Cromakalim-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELevcromakalimCat.No.:HY-14255CASNo.:94535-50-9Synonyms:(-)-Cromakalim;BRL38227分⼦式:C₁₆H₁₈N₂O₃分⼦量:286.33作⽤靶点:PotassiumChannel作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥50mg/mL(174.62mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4925mL17.4624mL34.9247mL5mM0.6985mL3.4925mL6.9849mL10mM0.3492mL1.7462mL3.4925mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.73mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.73mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Levcromakalim((-)-Cromakalim)ATP敏感性的K+通道(KATP)激活剂。IC50&TargetK+channel[1]体外研究Levcromakalim((-)-Cromakalim)inhibitsspontaneouscontractionscompletelyinaglibenclamide-sensitivemanner.LevCromakalim(5µM)inhibitsspontaneouscontractions,whicharerecoveredbyglibenclamide.Levcromakalim(1,5and10µM)inhibitsphasiccontractionsto34±21.1%,20.1±20.0%and0%ofthecontrol(n=5,respectively;P[2].ThefunctionoftheKATPchannelsisexaminedwiththespecificchannelopenerLevCromakalim(Cromakalim).LevCromakaliminducesdose-dependentrelaxationinboththeyoungandoldmesentericartery(MAs);andthereisnodifferenceinrelaxationwithage.However,therelaxationismarkedlyreducedinresponsetothehigh-salt(HS)dietintheoldMAs(P-4M)are97±3%intheyoungMAsversus98±1%intheyoungsaltarteries,whiledilationsare99±0.7%intheoldMAswhencomparedwith85±5%intheoldsaltarteries(P[3].PROTOCOLKinaseAssay[3]Levcromakalim(Cromakalim)isdissolvedin10%DMSOandKrebssolution[3].Theendothelium-dependentrelaxationistestedbyperformingconcentration-responseexperimentswithacetylcholine(ACh;10nM-10μM).Typically,MAsareexposedtoeachdoseofAChforatleast6minutesandmaximalresponsesaredetermined.FunctionoftheKATPchannelsareexaminedwith10µMofglibenclamide(aselectiveKATPchannelinhibitor)andLevcromakalim(Cromakalim)(10nMto100μM),aKATPchannelopener.Theadditionofglibenclamidetothearterialbath10minutespriortoAChdoesnotalterpassivemaximuminternaldiametersofanyMAsinourgroups.Thevesseldiameterchangesarepresentedaspercentages(%)ofdilationofthepreconstrictedvessels,calculated[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2022May13;13(1):2675.•JHeadachePain.2022Sep30;23(1):128.•Cephalalgia.2021Aug18;3331024211038884.•ResearchSquarePrint.August19th,2022.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].MatsumotoT,etal.Tunicamycin-InducedAlterationsintheVasorelaxantResponseinOrgan-CulturedSuperiorMesentericArteriesofRats.BiolPharmBull.2016;39(9):1475-81.[2].HongSH,etal.RegulationofmyometrialcontractionbyATP-sensitivepotassium(KATP)channelviaactivationofSUR2BandKir6.2inmouse.JVetMedSci.2016Aug1;78(7):1153-9.[3].WhiddenMA,AlteredpotassiumATPchannelsignalinginmesentericarteriesofoldhighsalt-fedrats.JExercNutritionBiochem.2016Jun;20(2):58-64.McePdfHeightCaution