Metformin-hydrochloride-1-1-Dimethylbiguanide-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMetforminhydrochlorideCat.No.:HY-17471ACASNo.:1115-70-4Synonyms:1,1-Dimethylbiguanidehydrochloride分⼦式:C₄H₁₂ClN₅分⼦量:165.62作⽤靶点:AMPK;Autophagy;Mitophagy作⽤通路:Epigenetics;PI3K/Akt/mTOR;Autophagy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(603.79mM)DMSO:≥1.7mg/mL(10.26mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM6.0379mL30.1896mL60.3792mL5mM1.2076mL6.0379mL12.0758mL10mM0.6038mL3.0190mL6.0379mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥3mg/mL(18.11mM);Clearsolution2.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥3mg/mL(18.11mM);Clearsolution3.请依序添加每种溶剂：PBSSolubility:100mg/mL(603.79mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Metforminhydrochloride(1,1-Dimethylbiguanidehydrochloride)抑制肝脏中的线粒体呼吸链，导致AMPK活化，增强胰岛素敏感性，可⽤于2型糖尿病的研究。Metforminhydrochloride可以透过⾎脑屏障，诱导⾃噬(autophagy)。IC50&TargetAMPK体外研究Metforminhydrochloride(1,1-Dimethylbiguanidehydrochloride)inhibitsproliferationofESCsinaconcentration-dependentmanner.TheIC50is2.45mMforA-ESCsand7.87mMforN-ESCs.MetforminshowspronouncedeffectsonactivationofAMPKsignalinginA-ESCsfromsecretoryphasethanincellsfromproliferativephase[2].Metforminhydrochloride(0-500μM)decreasesglycogensynthesisinadose-dependentmannerwithanIC50valueof196.5μMinculturedrathepatocytes[3].MetforminhydrochlorideshowscellviabilityandcytotoxiceffectsonPC-3cellswithIC50of5mM[4].体内研究Metforminhydrochloride(1,1-Dimethylbiguanidehydrochloride;100mg/kg,p.o.)alone,andmetformin(25,50,100mg/kg)withNSC37745groupsattenuatesmyocytenecrosisthroughhistopathologicalanalysis[1].PROTOCOLCellAssay[2]ESCsareplatedin96-wellplatesataconcentrationof1×103cells/well.Afterattachment,cellsaretreatedwithdifferentdosesofmetformin/compoundCfor0min,15min,1h,and24h.MTTassaysareperformedasdescribedpreviously.Inbrief,MTT(5mg/mL)isaddedtothe96-wellplatesatavolumeof10μL/well,andtheplatesareincubatedfor4h.TheMTTreactionisterminatedbyremovaloftheculturemediumcontainingMTT,and100μLDMSOperwellareaddedandincubatedatRTonashakerfor10mintoensurethatthecrystalshaddissolvedsufficiently.Absorbancevaluesaremeasuredat595nm.Cellproliferation(percentageofcontrol)iscalculatedasfollows:absorbance(experimentalgroup)/absorbance(controlgroup).Cellproliferationinhibition(percentageofcontrol)iscalculatedasfollows:100%−cellproliferation(percentageofcontrol).Eachexperimentisperformedinduplicateandrepeatedsixtimestoassessresultconsistency.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalTheanimalsarerandomizedintosixgroupsconsistingofsixratseach.Ratsingroup1(control)receivesaAdministration[1]subcutaneousinjectionofphysiologicalsaline(0.5mL)andareleftuntreatedfortheentireexperimental2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEperiod.Ratsingroup2receivesanoraladministrationofmetformin(100mg/kg;twicedaily)for2daysandaresubcutaneouslyinjectedwithsalineatanintervalof24hfor2consecutivedays.Ratsingroup3(MIcontrol)receivesanoraladministrationofsaline(twicedaily)for2daysandarescinjectedwithNSC37745(100mg/kg)dailyfor2consecutivedaysatanintervalof24h.Ratsingroups4to6aretreatedwithmetforminat25,50,and100mg/kg.Metforminisdissolvedinsalineandisgavagedatavolumeof0.25-0.5mLtwiceadayatanintervalof12h,startedimmediatelybeforeNSC37745injection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Circulation.2022Nov30.•CancerCell.2020Sep14;38(3):350-365.e7.•SignalTransductTargetTher.2020May20;5(1):56.•AdvMater.2020Nov;32(45):e2003708.•EmergMicrobesInfect.2022Feb22;1-34.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SorayaH,etal.AcutetreatmentwithmetforminimprovescardiacfunctionfollowingNSC37745inducedmyocardialinfarctioninrats.PharmacolRep.2012;64(6):1476-84.[2].XueJ,etal.MetformininhibitsgrowthofeutopicstromalcellsfromadenomyoticendometriumviaAMPKactivationandsubsequentinhibitionofAKTphosphorylation:apossibleroleinthetreatmentofadenomyosis.Reproduction.2013Aug21;146(4):397-406.[3].OttoM,etal.Metformininhibitsglycogensynthesisandgluconeogenesisinculturedrathepatocytes.DiabetesObesMetab.2003May;5(3):189-94.[4].AvciCB,etal.Therapeuticpotentialofananti-diabeticdrug,metformin:alterationofmiRNAexpressionin