PRX-07034-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPRX-07034hydrochlorideCat.No.:HY-14559CASNo.:903580-39-2分?式:C??H??Cl?N?O?S分?量:490.44作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:31.25mg/mL(63.72mM;ultrasonicandwarmingandheatto60°C)H2O:4.76mg/mL(9.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0390mL10.1949mL20.3899mL5mM0.4078mL2.0390mL4.0780mL10mM0.2039mL1.0195mL2.0390mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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:≥2.08mg/mL(4.24mM);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:≥2.08mg/mL(4.24mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.24mM);ClearsolutionBIOLOGICALACTIVITY?物活性PRX-07034hydrochloride?種有效的?度選擇性5-HT6受體拮抗劑，Ki為4-8nM，IC50為19nM。PRX-07034可?于增強(qiáng)?作記憶和認(rèn)知靈活性的研究[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)體外研究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].體內(nèi)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?邊的抑制劑?師www.MedChemE[1].EricGMohler,etal.TheeffectsofPRX-07034,anovel5-HT6antagonist,oncognitiveflexibilityandworkingmemoryinrats.Psychopharmacology(Berl).2012Apr;220(4):687-96.McePdfHeightCaution:Producthasnotbeenfullyvali