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Description | Metformin(hydrochloride)isafirst-linedrugforthetreatmentoftype2diabetesandthereisincreasingevidenceofapotentialefficacyofthisagentasananti-cancerdrug. |
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InVitro | MetformininhibitsproliferationofESCsinaconcentration-dependentmanner.TheIC50is2.45 mMforA-ESCsand7.87 mMforN-ESCs.MetforminshowspronouncedeffectsonactivationofAMPKsignalinginA-ESCsfromsecretoryphasethanincellsfromproliferativephase[3].Metformin(0-500μM)decreasesglycogensynthesisinadose-dependentmannerwithanIC50valueof196.5μMinculturedrathepatocytes[4].MetforminshowscellviABIlityandcytotoxiceffectsonPC-3cellswithIC50of5mM[5]. |
InVivo | Metformin(100mg/kg,p.o.)alone,andmetformin(25,50,100mg/kg)withisoproterenolgroupsattenuatesmyocytenecrosisthroughhistopathologicalanalysis[1].Metformin(>900mg/kg/day,p.o.)resultsinmoribundity/mortalityandclinicalsignsoftoxicityinCrl:CD(SD)rats[2]. |
ClinicalTrial | ViewMoreCollapse |
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Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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CellAssay [3] | Metforminisdissolvedindouble-distilledwateratastockconcentrationof10mMandstoredat4°C. 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. | ||||||||||||||||
AnimalAdmiNISTration [1] | Metformin(hydrochloride)isdissolvedinphysiologicalsaline. Theanimalsarerandomizedintosixgroupsconsistingofsixratseach.Ratsingroup1(control)receivesasubcutaneousinjectionofphysiologicalsaline(0.5mL)andareleftuntreatedfortheentireexperimentalperiod.Ratsingroup2receivesanoraladministrationofmetformin(100mg/kg;twicedaily)for2daysandaresubcutaneouslyinjectedwithsalineatanintervalof24hfor2consecutivedays.Ratsingroup3(MIcontrol)receivesanoraladministrationofsaline(twicedaily)for2daysandarescinjectedwithisoproterenol(100mg/kg)dailyfor2consecutivedaysatanintervalof24h.Ratsingroups4to6aretreatedwithmetforminat25,50,and100mg/kg.Metforminisdissolvedinsalineandisgavagedatavolumeof0.25-0.5mLtwiceadayatanintervalof12h,startedimmediatelybeforeisoproterenolinjection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
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MolecularWeight | 165.62 | ||||||||||||
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Formula | C₄H₁₂ClN₅ | ||||||||||||
CASNo. | 1115-70-4 | ||||||||||||
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | H2O:≥32mg/mL;DMSO:≥1.7mg/mL Metforminhydrochlorideispreparedin0.5%methylcellulose[6]. *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> | ||||||||||||
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Purity:99.08%