Agmatine-sulfate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAgmatinesulfateCat.No.:HY-101238CASNo.:2482-00-0分?式:C?H??N?O?S分?量:228.27作?靶點(diǎn):ImidazolineReceptor;NOSynthase;EndogenousMetabolite作?通路:NeuronalSignaling;Immunology/Inflammation;MetabolicEnzyme/Protease儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:≥100mg/mL(438.08mM)DMSO:1mg/mL(4.38mM;ultrasonicandwarmingandheatto80°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.3808mL21.9039mL43.8078mL5mM0.8762mL4.3808mL8.7616mL10mM0.4381mL2.1904mL4.3808mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：PBS1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:25mg/mL(109.52mM);Clearsolution;NeedultrasonicandwarmingBIOLOGICALACTIVITY?物活性Agmatinesulfate在多個(gè)靶點(diǎn)上發(fā)揮調(diào)節(jié)作?，如神經(jīng)遞質(zhì)系統(tǒng)，離?通道，?氧化氮合成。它imidazolinereceptor的內(nèi)性激動(dòng)劑和NOsynthase抑制劑。IC50&TargetHumanEndogenousMetabolite體外研究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].體內(nèi)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?邊的抑制劑?師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