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Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETempolCat.No.:HY-100561CASNo.:2226-96-2Synonyms:4-Hydroxy-TEMPO分⼦式:C₉H₁₈NO₂*分⼦量:172.24作⽤靶点:ReactiveOxygenSpecies;Autophagy作⽤通路:Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:5.56mg/mL(32.28mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.8059mL29.0293mL58.0585mL5mM1.1612mL5.8059mL11.6117mL10mM0.5806mL2.9029mL5.8059mL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:PBSSolubility:25mg/mL(145.15mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Tempol⼀种超氧化物歧化酶(SOD)类似物,可有效中和活性氧(ROS)。IC50&TargetROS[1]体外研究TempolsignificantlyattenuatesH2O2-mediateddecreaseinmitochondrialrespirationandincreaseinLDHreleasefromratPTcells,indicatingareductionincellinjuryanddeath.ThebeneficialactionsofTempolaresimilartothoseobtainedusingtheFe2+chelatorDEF.However,coadministrationofDEFandTempoldoesnotproduceanyadditionalbeneficialactionsagainstrenalischemia/reperfusioninjuryoragainstoxidativestress-mediatedPTcellinjury/death[2].体内研究SOD-mimeticTempolisabletomimicresveratrol’seffectsonheartfunction.Tempolisadministereddailybygavage.MicetreatedwithMetorTmphaddecreasedPRandQTcintervalsandincreasedheartratescomparedtoperoralvehicle(VEH).TheseresultsaresimilartothatobtainedbytreatmentwithRSV.Pre-andpost-treatmentprofilesofindividualmiceareillustrated[1].Tempol,amembrane-permeableradicalscavenger,reducesoxidantstress-mediatedrenaldysfunctionandinjuryintherat.Tempolsignificantlyreducestheincreaseinurea,creatinine,γGT,AST,NAG,andFENaproducedbyrenalischemia/reperfusion,suggestinganimprovementinbothrenalfunctionandinjury.TempolalsosignificantlyreduceskidneyMPOactivityandMDAlevels,indicatingareductioninPMNinfiltrationandlipidperoxidation,respectively.Tempolreducesthehistologicevidenceofrenaldamageassociatedwithischemia/reperfusionandcausedasubstantialreductioninthestainingfornitrotyrosineandPARS,suggestingreducednitrosativeandoxidativestress[2].PROTOCOLCellAssay[2]ToinvestigatetheeffectofTempol,DEF,andDEFcoadministeredwithTempolonH2O2-mediatedcellinjuryanddeath,confluentculturesofPTcellsarepreincubated(10minat37°C)withTempol(0.03to10mM),DEF(0.03to10mM),orDEF(3mM)incombinationwithTempol(3mM).TherangesofconcentrationsofTempolandDEFarebasedonthosepreviouslyshowninthislaboratorytoreduceonH2O2-mediatedcellinjuryanddeathin(1)culturedratcardiacmyoblasts(Tempol)and(2)primaryculturesofratPTcells(DEF).PTcellculturesarethenincubatedwithH2O2(1mM)forfourhours,afterwhichcellularinjuryanddeathareassessed.Uponcompletionofincubations,cellularinjuryanddeathareassessedusingthespectrophotometricassaysdescribedlaterinthisarticle[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1][2]FemaleormaleBALB/cmice(5-7weeksofage)areused.Miceareinfectedintraperitoneally(i.p.)with102bloodtrypomastigoteformsofthetypeIColombianstrainofT.cruzi.Treatmentsareperformeddailyfor302/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEdaysfromtheestablishmentofCCC(60dpi)byi.p.injectionof15mg/kgtrans-resveratrol(10%ethanol/PBS),vehicle(10%ethanol/PBS),5mg/KgEX527(0.1%DMSO),orperoraladministrationof40mg/KgResveratrol(10%ethanol-PBS),500mg/kgMetformin(dissolvedinwater),100mg/kgTempol(dissolvedinwater),Benznidazole(25mg/Kg,dissolvedinwater)andvehicle(wateror10%ethanol-PBS).Rats[2]83maleWistarratsweighing230to320gareused.Uponcompletionofsurgicalprocedures,theanimalsarerandomlyallocatedtotheeightgroups.Atoneminutebeforecommencementofreperfusion,animalsreceivedabolusinjectionofeithervehicle(saline,4mL/kg,IV),Tempol(30mg/kginsaline,IV),DEF(40mg/kginsaline,IV),orDEF(40mg/kginsaline,IV)incombinationwithTempol(30mg/kginsaline,IV).Thecorrespondinggroupsthenreceivedacontinuousinfusionofoneofthefollowingthroughoutthereperfusionperiod:vehicle(saline,4mL/kg/h,IV),Tempol(30mg/kg/hinsaline,IV),DEF(40mg/kg/hinsaline,IV),orTempolandDEFincombination(30and40mg/kg/h,respectively,insaline,IV).ToelucidatetheeffectsofTempolorDEFoncardiovascularhemodynamicsandorganfunctioninsham-operatedrats,respectivegroupsofanimalsreceivedthetreatmentsdescribedpreviouslyinthisarticleandasoutlined.TheconcentrationofTempoladministeredinvivoisbasedonthosepreviouslydemonstratedbyustoprovidesignificantprotectionagainstmyocardialischemia/reperfusioninjuryinaninvivoratmodel.Similarly,theconcentrationofDEFusedisidenticaltothatwhichwehavepreviouslyusedtoprovidesignificantprotectionagainsthepaticischemia/reperfusioninjuryininvivoratandrabbitmodels.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•RedoxBiol.October2021,102115.•Cells.2022Apr2;11(7):1196.•OxidMedCellLongev.05Oct2021.•JNutrBiochem.2021Oct1
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