Agmatine-sulfate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAgmatinesulfateCat.No.:HY-101238CASNo.:2482-00-0分⼦式:C₅H₁₆N₄O₄S分⼦量:228.27作⽤靶点:ImidazolineReceptor;NOSynthase;EndogenousMetabolite作⽤通路:NeuronalSignaling;Immunology/Inflammation;MetabolicEnzyme/Protease储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:≥100mg/mL(438.08mM)DMSO:1mg/mL(4.38mM;ultrasonicandwarmingandheatto80°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM4.3808mL21.9039mL43.8078mL5mM0.8762mL4.3808mL8.7616mL10mM0.4381mL2.1904mL4.3808mL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(sealedstorage,awayfrommoisture)。-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.请依序添加每种溶剂：PBS1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:25mg/mL(109.52mM);Clearsolution;NeedultrasonicandwarmingBIOLOGICALACTIVITY⽣物活性Agmatinesulfate在多个靶点上发挥调节作⽤，如神经递质系统，离⼦通道，⼀氧化氮合成。它imidazolinereceptor的内性激动剂和NOsynthase抑制剂。IC50&TargetHumanEndogenousMetabolite体外研究Agmatinebindstoalpha2-adrenergicandimidazolinereceptorsandstimulatesreleaseofcatecholaminesfromadrenalchromaffincells.Itsbiosyntheticenzyme,argininedecarboxylase,ispresentinbrain.Agmatine,locallysynthesized,isanendogenousagonistatimidazolinereceptors,anoncatecholamineligandatalpha2-adrenergicreceptorsandmayactasaneurotransmitter[1].Agmatineissynthesizedinthebrain,storedinsynapticvesiclesinregionallyselectiveneurons,accumulatedbyuptake,releasedbydepolarization,andinactivatedbyagmatinase.Agmatineinhibitsnitricoxidesynthase,andinducesthereleaseofsomepeptidehormones[2].Agmatine,4-(aminobutyl)guanidine,isproducedbydecarboxylationofL-argininebytheenzymeargininedecarboxylase.AgmatineisacompetitiveinhibitorofallNOSisoenzymesbutnotanNOprecursor.Kivaluesareapproximately660µM(NOSI),220µM(NOSII)and7.5mM(NOSIII)[3].Agmatinestimulatesnitriteproductionthree-foldabovebasalnitriteformationbyendothelialcells.Agmatinedisplaces[3H]-idazoxanfromendothelialcellmembranesandisfoundtoinducetransientsinthecytosoliccalciumofendothelialcells.Thetransientscouldbedownregulatedbyrepeatedexposuretoagmatinebutarenotaffectedbypretreatmentwithnorepinephrine[4].体内研究Agmatineproducesanantidepressant-likeeffectwhenassessedintheforcedswimmingtestandinthetailsuspensiontestinmice(doserange0.01-50mg/kg,i.p.),withoutaccompanyingchangesinambulationinanopen-field[5].Inischemicstroke,agmatineprotectstheblood-brainbarrier,whichcanbemonitoredinvivobyquantificationofpermeabilitybyusingdynamiccontrast-enhancedMRimaging[6].Agmatinesubstantiallyaugmentstheantidepressant-likeeffectofMK-801,reinforcingthenotionthatthiscompoundmodulatesNMDAreceptoractivation[7].PROTOCOLAnimalRats:Thirty-fourmaleSprague-DawleyratsaresubjectedtotransientMCAocclusionfor90minutes.Administration[6][7]Immediatelyafterreperfusion,agmatine(100mg/kg)ornormalsalineisinjectedintraperitoneallyintotheagmatine-treatedgroup(n=17)orthecontrolgroup,respectively.MRimagingisperformedafterreperfusion[6].Mice:Micearepretreatedwitharangeofsub-effectivedosesofeitherfluoxetine(1,2.5and5mg/kg,p.o.;aselectiveserotoninreuptakeinhibitor),imipramine(0.01,0.05and0.1mg/kg,p.o.;atricyclicantidepressant),bupropion(0.1,0.5and1mg/kg,p.o.;dopaminereuptakeinhibitorwithsubtleactivityonnoradrenergicreuptake),orMK-801(0.0001,0.0005and0.001mg/kg,p.o.;noncompetitiveNMDAreceptorantagonist)andimmediatelyafter,asub-effectivedoseofeitheragmatine(0.0001mg/kgp.o.)orvehicleisadministered.After60min,theanimalsaresubjectedtobehavioraltesting[7].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].LiG,etal.Agmatine:anendogenousclonidine-displacingsubstanceinthebrain.Science.1994Feb18;263(5149):966-9.[2].ReisDJ,etal.Isagmatineanovelneurotransmitterinbrain?TrendsPharmacolSci.2000May;21(5):187-93.[3].GaleaE,etal.Inhibitionofmammaliannitricoxidesynthasesbyagmatine,anendogenouspolyamineformedbydecarboxylationofarginine.BiochemJ.1996May15;316(Pt1):247-9.[4].MorrisseyJJ,etal.Agmatineactivationofnitricoxidesynthaseinendothelialcells.ProcAssocAmPhysicians.1997Jan;109(1):51-7.[5].ZomkowskiAD,etal.Agmatineproducesantidepressant-likeeffectsintwomodelsofdepressioninmice.Neuroreport.2002Mar25;13(4):387-91.[6].AhnSS,etal.Effectsofagmatineonblood-brainbarrierstabilizationassessedbypermeabilityMRIinaratmodeloftransientcerebralischemia.AJNRAmJNeuroradiol.2015Feb;36(2):283-8.[7].NeisVB,etal.AgmatineenhancesantidepressantpotencyofMK-801andconventionalantid