CDN1163-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECDN1163Cat.No.:HY-101455CASNo.:892711-75-0分?式:C??H??N?O?分?量:320.39作?靶點(diǎn):CalciumChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(312.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1212mL15.6060mL31.2120mL5mM0.6242mL3.1212mL6.2424mL10mM0.3121mL1.5606mL3.1212mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.80mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.80mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性CDN1163?種肌膜/內(nèi)質(zhì)?Ca2+-ATPase(SERCA)的變構(gòu)激活劑，可改Ca2+穩(wěn)態(tài)。CDN1163可減輕糖尿病和代謝紊亂。IC50&TargetSERCA[1]體外研究CDN1163(10?μM;24hours;ratcardiacmyocytecells)treatmentreduceshighglucose-inducedresistinandnuclearNFATcexpressionandincreasesthephosphorylationofAMPKαinatime-dependentmanner[2].WesternBlotAnalysis[2]CellLine:Ratcardiacmyocytecells(H9c2)Concentration:10?μMIncubationTime:24hoursResult:Highglucose-inducedresistinandnuclearNFATcexpressionaresignificantlyreduced.ThephosphorylationofAMPKαisincreasedinatime-dependentmanner.體內(nèi)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?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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