IM156-HL156A-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEIM156Cat.No.:HY-136093ACASNo.:1422365-94-3Synonyms:HL156A;HL271acetate分⼦式:C₁₅H₂₀F₃N₅O₃分⼦量:375.35作⽤靶点:AMPK作⽤通路:Epigenetics;PI3K/Akt/mTOR储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(266.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6642mL13.3209mL26.6418mL5mM0.5328mL2.6642mL5.3284mL10mM0.2664mL1.3321mL2.6642mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.66mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.66mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoil1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.66mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性IM156(HL156A;HL271acetate)⼆甲双胍(HY-B0627)的化学衍⽣物，⼀种强效的AMPK激活剂。IM156在动物模型中可缓解与年龄相关的认知障碍[1][2]。IM156⼀种有效的氧化磷酸化(OXPHOS)抑制剂，可⽤于实体肿瘤的研究[3]。IC50&TargetAMPK[1][2],OXPHOS[3]体外研究IM156(0.31-10μM)phosphorylatesAMPKα1Thr172inadose-andtime-dependentmannerinNIH3T3mousefibroblastcells[1].IM156doesnotaffecttheexpressionofkeyfactorsinvolvedinglucosehomeostasissuchasglucose-6-phosphatase(G6pase)orphosphoenolpyruvatecarboxykinase1(Pck1)[1].WesternBlotAnalysis[1]CellLine:NIH3T3cellsConcentration:0.31μM,0.62μM,1.25μM,2.5μM,5μM,10μMIncubationTime:4hoursResult:SignificantlyincreasedtheAMPKphosphorylationrate.体内研究IM156doesnotaffectmetabolicregulationassessedbybodyweight,bloodglucose,insulinlevelsandlipidmetabolitecontentinmicewithdiet-inducedobesity[1].IM156(50mg/kg;for2months)doesnotaffectbodyweight,generallocomotion,oranxiety[2].IM156significantlyattenuatestheaging-induceddeclineinnovelobjectrecognitionmemoryandspatialworkingmemory[2].IM156significantlyincreasesAMPKactivationinthehippocampusofagedmice[2].AnimalModel:C57BL/6Jmice(younggroup/12-16weeks,oldgroups/20-22months)[2]Dosage:50mg/kgAdministration:Oraladministration(drinkingwater),for2monthsResult:Attenuatedage-relatedcognitivedecline.REFERENCES[1].RowH,etal.HL271,anovelchemicalcompoundderivedfrommetformin,differsfrommetformininitseffectsonthecircadianclockandmetabolism.BiochemBiophysResCommun.2016Jan15;469(3):783-9.2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].BangE,etal.TheImprovingEffectofHL271,aChemicalDerivativeofMetformin,aPopularDrugforTypeIIDiabetesMellitus,onAging-inducedCognitiveDecline.ExpNeurobiol.2018Feb;27(1):45-56.[3].SunYoungRha,etal.PhaseIstudyofIM156,anovelpotentbiguanideoxidativephosphorylation(OXPHOS)inhibitor,inpatientswithadvancedsolidtumors.JournalofClinicalOncology38(15_suppl):3590-3590.McePdfHeightCaution:Producthasnotbeenfullyval