CDN1163-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECDN1163Cat.No.:HY-101455CASNo.:892711-75-0分⼦式:C₂₀H₂₀N₂O₂分⼦量:320.39作⽤靶点:CalciumChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(312.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1212mL15.6060mL31.2120mL5mM0.6242mL3.1212mL6.2424mL10mM0.3121mL1.5606mL3.1212mL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:≥2.5mg/mL(7.80mM);Clearsolution1/3MasterofBioactiveMolecules—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:2.5mg/mL(7.80mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.80mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CDN1163⼀种肌膜/内质⽹Ca2+-ATPase(SERCA)的变构激活剂，可改Ca2+稳态。CDN1163可减轻糖尿病和代谢紊乱。IC50&TargetSERCA[1]体外研究CDN1163(10ꢀμM;24hours;ratcardiacmyocytecells)treatmentreduceshighglucose-inducedresistinandnuclearNFATcexpressionandincreasesthephosphorylationofAMPKαinatime-dependentmanner[2].WesternBlotAnalysis[2]CellLine:Ratcardiacmyocytecells(H9c2)Concentration:10ꢀμMIncubationTime:24hoursResult:Highglucose-inducedresistinandnuclearNFATcexpressionaresignificantlyreduced.ThephosphorylationofAMPKαisincreasedinatime-dependentmanner.体内研究CDN1163(50mg/kg;intraperitonealinjection;for5days;maleob/obmiceandleanob/+mice)increasesSERCA2Ca2+-ATPaseactivity,decreasesendoplasmicreticulum(ER)stress-inducedcelldeathinvitroandimprovesliverCa2+transportactivity.CDN1163reducesbloodglucoselevelsandimprovesmetabolicparametersandgluconeogenicgeneexpression,reverseshepaticsteatosis,inhibitsERstressandERstress-inducedapoptosis,andimprovesmitochondrialefficiencyinob/obmiceinvivo[1].AnimalModel:Male8-10-weekoldob/obmiceandleanob/+mice[1]Dosage:50mg/kgAdministration:Intraperitonealinjection;for5daysResult:Markedlyloweredfastingbloodglucose,improvedglucosetolerance,andamelioratedhepatosteatosisbutdidnotalterglucoselevelsorbodyweight.Increasedexpressionofuncouplingprotein1(UCP1)andUCP3inbrownadiposetissueandreducedthehepaticexpressionofgenesinvolvedingluconeogenesisandlipogenesis,attenuatedERstressresponseandERstress-inducedapoptosis,andimprovedmitochondrialbiogenesis,possiblythroughSERCA2-mediatedactivationofAMP-activatedproteinkinasepathway.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•JHazardMater.2021,126025.•JVirol.2021Mar10;JVI.00217-21.•BiochemPharmacol.2022Jul6;115164.•BehavBrainRes.2021Feb5;399:112984.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KangS,etal.SmallMolecularAllostericActivatoroftheSarco/EndoplasmicReticulumCa2+-ATPase(SERCA)AttenuatesDiabetesandMetabolicDisorders.JBiolChem.2016Mar4;291(10):5185-98.[2].SinghR,etal.Aroleforcalciuminresistintranscriptionalactivationindiabetichearts.SciRep.2018Oct23;8(1):15633.McePdfHeightCaution:Productha