AZD1656-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAZD1656Cat.No.:HY-15675CASNo.:919783-22-5分⼦式:C₂₄H₂₆N₆O₅分⼦量:478.5作⽤靶点:Glucokinase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:250mg/mL(522.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0899mL10.4493mL20.8986mL5mM0.4180mL2.0899mL4.1797mL10mM0.2090mL1.0449mL2.0899mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.35mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.35mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.35mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AZD1656⼀种有效的，选择性的，具有⼝服活性的葡萄糖激酶(glucokinase)激活剂，EC50为60nM，可⽤于2型糖尿病的研究。IC50&TargetEC50:60nM(Glucokinase)[2]体内研究AZD1656(0-9mg/kg;oralgavage;daily;for8weeks;C57BL/6mice)treatmentshowsloweredbloodglucoseandglucoseexcursionandraisedinsulin.LivermRNAlevelsforvariousChREBPtargetgenesincludingcarbohydrateresponseelementbindingproteinbetaisoform(ChREBP-β),G6pc,Pklr,Acly,AcacandGpd2areincreasedbyAZD1656[1].AnimalModel:C57BL/6mice[1]Dosage:0mg/kg,2mg/kg,4.5mg/kg,9mg/kgAdministration:Oralgavage;daily;for8weeksResult:Administered2hoursbeforetheoralglucosetolerancetest,loweredbloodglucoseandglucoseexcursionandraisedinsulin.REFERENCES[1].BrianEFord,etal.ChronicglucokinaseactivatortreatmentactivatesliverCarbohydrateresponseelementbindingproteinandimproveshepatocyteATPhomeostasisduringsubstratechallenge.DiabetesObesMetab.2020Jun10.[2].MedicinalChemistry,etal.DesignandDevelopmentoftheGlucokinaseActivatorAZD1656.CompleteAccountsofIntegratedDrugDiscoveryandDevelopment:RecentExamplesfromthePharmaceuticalIndustryVolume1,185-220.[3].TerriMitchard,etal.Thenoveluseofaheterozygousknockoutmouseforembryofetaldevelopmentassessmentofaglucokinaseactivator.BirthDefectsResBDevReprodToxicol.2014Apr;101(2):152-61.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications