Alogliptin-SYR-322-free-base-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAlogliptinCat.No.:HY-A0023ACASNo.:850649-61-5Synonyms:SYR-322freebase分⼦式:C₁₈H₂₁N₅O₂分⼦量:339.39作⽤靶点:DipeptidylPeptidase;Ferroptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(294.65mM;Needultrasonic)H2O:10mg/mL(29.46mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9465mL14.7323mL29.4646mL5mM0.5893mL2.9465mL5.8929mL10mM0.2946mL1.4732mL2.9465mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.37mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.37mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.37mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Alogliptin(SYR-322freebase)⼀种有效的、具有选择性⼝服活性的DPP-4的抑制剂，IC50值⼩于10nM，⽐对DPP-8和DPP-9的抑制性⾼10000倍以上。Alogliptin可⽤于研究2型糖尿病。IC50&TargetIC50:[1]体外研究Alogliptin(1nM;5-60min)inhibitsLPS-inducedextracellularsignal-regulatedkinase(ERK)phosphorylationinU937cells[2].Alogliptin(0.5-5nM;24h)inhibitsLPS-stimulatedMMP-1secretionandmRNAexpressionthatismediatedbyERKpathwayinU937cells[2].体内研究Alogliptin(0.01-1mg/kg;p.o.)produceddose-dependentimprovementsinglucosetoleranceandincreasedplasmainsulinlevelsinfemaleWistarfattyrats[1].Alogliptin(40ꢀmg/kg/dayfor2weeks;p.o.)reducesinfarctionareaandimprovesbrainvascularintegrityinmiddlecerebralarteryocclusion(MCAO)mice[3].户使⽤本产品发表的科研⽂献•SciRep.2019Dec2;9(1):18094.•BiochemBiophysResCommun.2019Apr2;511(2):387-393.•Chromatography.2015,36(1):19-24.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FengJ,etal.Discoveryofalogliptin:apotent,selective,bioavailable,andefficaciousinhibitorofdipeptidylpeptidaseIV.JMedChem.2007May17;50(10):2297-300.[2].TaNN,etal.DPP-4(CD26)inhibitoralogliptininhibitsTLR4-mediatedERKactivationandERK-dependentMMP-1expressionbyU937histiocytes.Atherosclerosis.2010Dec;213(2):429-35.[3].AsakawaT,etal.Anoveldipeptidylpeptidase-4inhibitor,alogliptin(SYR-322),iseffectiveindiabeticratswithsulfonylurea-inducedsecondaryfailure.LifeSci.2009Jul17;85(3-4):122-6.[4].MoritohY,etal.Thedipeptidylpeptidase-4inhibitoralogliptinincombinationwithpioglitazoneimprovesglycemiccontrol,lipidprofiles,andincreasespancreaticinsulincontentinob/obmice.EurJPharmacol.2009Jan14;602(2-3):448-54.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[5].HaoFL,et,al.TheneurovascularprotectiveeffectofalogliptininmurineMCAOmodelandbrainendothelialcells.BiomedPharmacother.2019Jan;109:181-187.McePdfHeightCaution:Producthasnotbeenfull