SUVN-911-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESUVN-911Cat.No.:HY-136146CASNo.:2414674-71-6分⼦式:C₁₁H₁₄Cl₂N₂O分⼦量:261.15作⽤靶点:nAChR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:125mg/mL(478.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8292mL19.1461mL38.2922mL5mM0.7658mL3.8292mL7.6584mL10mM0.3829mL1.9146mL3.8292mL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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性SUVN-911⼀种⾼效、选择性的，有⼤脑通透性和⼝服⽣物活性的神经元烟碱⼄酰胆碱α4β2受体(α4β2receptor)拮抗剂，Ki值为1.5nM。SUVN-911具有抗抑郁作⽤[1]。IC50&TargetKi:1.5nM(α4β2receptor)[1]体外研究SUVN-911displayshighselectivityforα4β2overα3β4nAChR[1].SUVN-911showsgoodselectivityagainstover70receptorswhichincludesGPCRs,ionchannels,enzymes,1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEpeptides,steroids,secondmessengers,growthfactorsandprostaglandins[1].体内研究SUVN-911isdevoidofcardiovascularandgastrointestinalsideeffects[1].SUVN-911(1.0-10.0mg/kg;p.o.;daily;for3days)showssignificantantidepressanteffects[1].SUVN-911showsmetabolicstabilityinrats[1].SUVN-911(3mg/kg;p.o.)hasshownhighoralexposures,longerhalf-livesandadequatebrainpenetrationinWistarrats[1].AnimalModel:MaleWistarrats(180-230g)[1]Dosage:1mg/kg,3mg/kg,10.0mg/kgAdministration:Oraladministration,daily,for3daysResult:Showedantidepressantlikeactivitywithnosignsoftachyphylaxis.AnimalModel:MaleWistarrats(225±25g)[1]Dosage:3mg/kg(PharmacokineticAnalysis)Administration:OraladministrationResult:AUC=3507ng*h/mL,T1/2=3.34hours.REFERENCES[1].RamakrishnaNirogi,etal.DiscoveryandDevelopmentof3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexaneHydrochloride(SUVN-911):ANovel,Potent,Selective,andOrallyActiveNeuronalNicotinicAcetylcholineα4β2ReceptorAntagonistfortheTreatmentofDepression.JMedChem.2020Mar26;63(6):2833-2853.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl