Vildagliptin-LAF237-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVildagliptinCat.No.:HY-14291CASNo.:274901-16-5Synonyms:LAF237;NVP-LAF237分?式:C??H??N?O?分?量:303.4作?靶點(diǎn):DipeptidylPeptidase;Ferroptosis;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:50mg/mL(164.80mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2960mL16.4799mL32.9598mL5mM0.6592mL3.2960mL6.5920mL10mM0.3296mL1.6480mL3.2960mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：PBS1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:100mg/mL(329.60mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性Vildagliptin(LAF237)?種有效且穩(wěn)定的選擇性?肽肽酶IV(DPP-IV)抑制劑，在?Caco-2細(xì)胞中抑制DPP-IV的IC50為3.5nM。Vildagliptin具有出?的?服?物利?度和有效的降?糖活性[1]。IC50&TargetIC50:3.5nM(DPP-IV,inhumanCaco-2cells)[1]體外研究Vildagliptinpromotesbetacellsurvivalbyinhibitingcellapoptosis.Vildagliptinalsopromotescellproliferation[2].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemEdipeptidylpeptidaseIVinhibitorwithantihyperglycemicproperties.JMedChem.2003Jun19;46(13):2774-89.[2].WuYJ,etal.Dipeptidylpeptidase-4inhibitor,vildagliptin,inhibitspancreaticbetacellapoptosisinassociationwithitseffectssuppressingendoplasmicreticulumstressindb/dbmice.Metabolism.2015Feb;64(2):226-35.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap