SDMA-Symmetric-dimethylarginine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESDMACat.No.:HY-101410CASNo.:30344-00-4Synonyms:Symmetricdimethylarginine;NG,NG'-Dimethyl-L-arginine分⼦式:C₈H₁₈N₄O₂分⼦量:202.25作⽤靶点:EndogenousMetabolite作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:67.5mg/mL(333.75mM;Needultrasonic)H2O:50mg/mL(247.22mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.9444mL24.7219mL49.4438mL5mM0.9889mL4.9444mL9.8888mL10mM0.4944mL2.4722mL4.9444mL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(12.36mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(12.36mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.5mg/mL(12.36mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：PBSSolubility:120mg/mL(593.33mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性SDMA(Symmetricdimethylarginine)⼀氧化氮(NO)合酶活性的内性抑制剂。IC50&TargetHumanEndogenousMetabolite体外研究SDMAisthestructuralisomerofthecardiovascularriskmarkerasymmetricdimethylarginine,asanendogenousmarkerofrenalfunction.SDMAdoesnotdirectlyinhibitNOSbutisacompetitorofargininetransport.SDMAisprimarilyeliminatedbyrenalexcretionandisapromisingendogenousmarkerofglomerularfiltrationrate[1].SDMAinhibitsdosedependentlytheNOsynthesisinintactendothelialcells,whereasithasnoeffectonproteinexpressionofNOS[1].SDMAisinvolvedintheinflammatoryprocessofchronickidneydisease,activatingNF-κBandresultinginenhancedexpressionofIL-6andTNF-α[2].体内研究SDMAishighlystableinserumandplasma,andtheassaydemonstratesexcellentanalyticalperformance.Inunaffecteddogs,SDMAremainsunchangedwhereasinaffecteddogs,SDMAincreasesduringdiseaseprogression,correlatingstronglywithanincreaseinsCranddecreaseinGFR[3].ChronicSDMAinfusionleadstoasignificantincreaseofSDMAlevelsinmice,buttheGFRdidnotchangeat4weeks.Nohistologicalchangesareobserved,particularlynoeffectonfibrosisorendotheliasnitricoxidesynthaseexpression.ThereisneitheraneffectofSDMAonsystolicbloodpressurenoronejectionfraction[4].PROTOCOLCellAssay[2]SDMAstocksolutionispreparedin0.9%NaClanddilutedinthecellculturemediumorinheparinizedwholebloodresultinginamaximaluremicconcentrationof6.1μMSDMA.Wholebloodisincubatedwithsaline(control)ordifferentdosesofADMA(0.6,3.6,and36μM)orSDMA(1.5,3.1,and6.1μM)for2hoursinahumidifiedatmosphereof5%CO2inairat37°C.CellsarefinallystainedforintracellularTNF-αorIL-6.Samplesareanalyzedwithaflowcytometer[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Eight-week-oldmaleC57Bl/6micereceivesvehicle-controlledinfusionofSDMA(250µmol/kg/days)forAdministration[4]28daysusingosmoticminipumps(n=24/group).Glomerularfiltrationrate,cardiacfunctionandbloodpressurearemonitored.BloodsamplesforSDMAdeterminationareobtainedatbaseline,2and4weeks.Miceareeuthanizedat4weekstoobtaintissueforrenalhistology[4].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].Bode-BögerSM,etal.Symmetricaldimethylarginine:anewcombinedparameterforrenalfunctionandextentofcoronaryarterydisease.[2].SchepersE,etal.Symmetricdimethylarginineasaproinflammatoryagentinchronickidneydisease.ClinJAmSocNephrol.2011Oct;6(10):2374-83.[3].NabityMB,etal.SymmetricDimethylarginineAssayValidation,Stability,andEvaluationasaMarkerfortheEarlyDetectionofChronicKidneyDiseaseinDogs.JVetInternMed.2015Jul-Aug;29(4):1036-44.[4].VeldinkH,etal.EffectsofchronicSDMAinfusiononglomerularfiltrationrate,bloodpressure,myocardialfunctionandrenalhistologyinC57BL6/Jmice.NephrolDialTransplant.20