PRX-07034-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPRX-07034hydrochlorideCat.No.:HY-14559CASNo.:903580-39-2分⼦式:C₂₁H₂₉Cl₂N₃O₄S分⼦量:490.44作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:31.25mg/mL(63.72mM;ultrasonicandwarmingandheatto60°C)H2O:4.76mg/mL(9.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0390mL10.1949mL20.3899mL5mM0.4078mL2.0390mL4.0780mL10mM0.2039mL1.0195mL2.0390mL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:≥2.08mg/mL(4.24mM);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:≥2.08mg/mL(4.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.24mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PRX-07034hydrochloride⼀种有效的⾼度选择性5-HT6受体拮抗剂，Ki为4-8nM，IC50为19nM。PRX-07034可⽤于增强⼯作记忆和认知灵活性的研究[1]。IC50&Target5-HT6Receptor5-HT6Receptor5-HT1AReceptor5-HT1BReceptor4-8nM(Ki)19nM(IC50)420nM(Ki)260nM(Ki)5-HT1DReceptor5-HT2AReceptor5-HT2BReceptor5-HT2CReceptor2.8μM(Ki)2.5μM(IC50)2.5μM(IC50)3.7μM(IC50)DopamineD3ReceptorHistamineH2OpioidμReceptor71nM(Ki)Receptor0.45μM(Ki)0.64μM(Ki)体外研究PRX-07034isbothapotentandhighlyselective5-HT6receptorantagonist(≥100-foldselectivityforthe5-HT6receptorcomparedto68otherGPCRs,ionchannels,andtransporters.PRX-07034inhibits5-HT1A,5-HT1B,5-HT1D,DopamineD3,HistamineH2,andOpioidμreceptorwithKisof420nM,260nM,2.8µM,71nM,0.64µM,and0.45µM,respectively.PRX-07034inhibits5-HT2A,5-HT2B,and5-HT2CreceptorswithIC50sof2.5µM,2.5µM,and3.7µM,respectively[1].Infunctionalassays,PRX-07034demonstrateslowantagonistactivityforthedopamineD3receptor(IC50=4.8µM)andverylowagonisticactivityfortheopioidμ-receptor(EC50=19µM)[1].体内研究PRX-07034(0.1,1,or3mg/kg;i.p.;30minpriortodelayedspontaneousalternationtesting)selectivelyenhancesaswitchtoaplacediscrimination[1].AnimalModel:MaleLong-Evansratsweighingapproximately350g[1]Dosage:0.1,1,or3mg/kgAdministration:InjectedintraperitonealResult:1and3mg/kg(butnot0.1mg/kg)significantlyenhanceddelayedspontaneousalternation.Thedrugat1and3mg/kgalsoenhancedswitchingbetweenaplaceandresponsestrategy,butdidnotaffectinitiallearningofeitheraplaceorresponsediscrimination.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].EricGMohler,etal.TheeffectsofPRX-07034,anovel5-HT6antagonist,oncognitiveflexibilityandworkingmemoryinrats.Psychopharmacology(Berl).2012Apr;220(4):687-96.McePdfHeightCaution:Producthasnotbeenfullyvali