Vildagliptin-LAF237-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVildagliptinCat.No.:HY-14291CASNo.:274901-16-5Synonyms:LAF237;NVP-LAF237分⼦式:C₁₇H₂₅N₃O₂分⼦量:303.4作⽤靶点:DipeptidylPeptidase;Ferroptosis;Apoptosis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H2O:50mg/mL(164.80mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2960mL16.4799mL32.9598mL5mM0.6592mL3.2960mL6.5920mL10mM0.3296mL1.6480mL3.2960mL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：PBS1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:100mg/mL(329.60mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性Vildagliptin(LAF237)⼀种有效且稳定的选择性⼆肽肽酶IV(DPP-IV)抑制剂，在⼈Caco-2细胞中抑制DPP-IV的IC50为3.5nM。Vildagliptin具有出⾊的⼝服⽣物利⽤度和有效的降⾎糖活性[1]。IC50&TargetIC50:3.5nM(DPP-IV,inhumanCaco-2cells)[1]体外研究Vildagliptinpromotesbetacellsurvivalbyinhibitingcellapoptosis.Vildagliptinalsopromotescellproliferation[2].体内研究Vildagliptin(35mg/kg;oncedailybyoralgavage)increasesplasmaactiveGLP-1levelsinisletsofdb/dbmice[2].Vildagliptin(10µmol/kg;orally)significantlydecreasesglucoseexcursionsandstimulateinsulinsecretioninobesemaleZuckerrats[1].AnimalModel:Maledb/dbmice(BKS)andwildtypemice[2]Dosage:35mg/kgAdministration:Oralgavage;oncedaily;for6weeksResult:IncreasedplasmaactiveGLP-1levels(22.63±1.19vs.11.69±0.44).AnimalModel:ObesemaleZuckerrats[1]Dosage:10µmol/kg(PharmacokineticAnalysis)Administration:OrallyResult:Significantlydecreasedglucoseexcursionsandstimulateinsulinsecretion.户使⽤本产品发表的科研⽂献•CancerLett.2018Apr28;420:26-37.•IntJMolSci.2022,23(22),14101•JBiolChem.2018Dec7;293(49):18864-18878.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].VillhauerEB,etal.1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine:apotent,selective,andorallybioavailable2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEdipeptidylpeptidaseIVinhibitorwithantihyperglycemicproperties.JMedChem.2003Jun19;46(13):2774-89.[2].WuYJ,etal.Dipeptidylpeptidase-4inhibitor,vildagliptin,inhibitspancreaticbetacellapoptosisinassociationwithitseffectssuppressingendoplasmicreticulumstressindb/dbmice.Metabolism.2015Feb;64(2):226-35.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap