IM156-HL156A-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEIM156Cat.No.:HY-136093ACASNo.:1422365-94-3Synonyms:HL156A;HL271acetate分?式:C??H??F?N?O?分?量:375.35作?靶點(diǎn):AMPK作?通路:Epigenetics;PI3K/Akt/mTOR儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(266.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6642mL13.3209mL26.6418mL5mM0.5328mL2.6642mL5.3284mL10mM0.2664mL1.3321mL2.6642mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.66mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.66mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoil1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.66mM);ClearsolutionBIOLOGICALACTIVITY?物活性IM156(HL156A;HL271acetate)?甲雙胍(HY-B0627)的化學(xué)衍?物，?種強(qiáng)效的AMPK激活劑。IM156在動物模型中可緩解與年齡相關(guān)的認(rèn)知障礙[1][2]。IM156?種有效的氧化磷酸化(OXPHOS)抑制劑，可?于實體腫瘤的研究[3]。IC50&TargetAMPK[1][2],OXPHOS[3]體外研究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.體內(nèi)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?邊的抑制劑?師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