DuP-734-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEDuP734Cat.No.:HY-136281CASNo.:135135-87-4分⼦式:C₁₇H₂₃BrFNO分⼦量:356.27作⽤靶点:SigmaReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,storedundernitrogen,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen,awayfrommoisture)溶解性数据体外实验DMSO:250mg/mL(701.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8069mL14.0343mL28.0686mL5mM0.5614mL2.8069mL5.6137mL10mM0.2807mL1.4034mL2.8069mL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。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.84mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.84mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.84mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性DuP734⼀种sigma受体拮抗剂，DuP734⼀种有效的选择性sigma和5-HT2受体配体，对D2受体的亲和⼒弱。DuP734具有抗精神病活性，⽽没有抗精神病剂常见的副作⽤[1][2][3]。IC50&TargetSigmareceptor;5-HT2receptor;D2receptor[1][2][3]体内研究DuP734potentlyblocksmescaline-inducedscratching(ED50=0.35mg/kg,p.o.)andaggressiveactivity(ED50=1.9mg/kg,p.o.)andisrelativelymuchweakerasanapomorphineantagonist(ED50=12mg/kg,p.o.)[1].AdministrationofDuP734potentlyantagonizesthebindingof[3H]DuP734and[3H](+)-SKF10,047tobrainsigmareceptorsinvivowithID50valuesof0.02and0.07mg/kg(0.07and0.25μmol/kg),respectively[2].Followingintravenousdosing,thedispositionofDuP734inmice,rats,beagledogsandcynomolgusmonkeysischaracterizedbyhightotalbodysystemicplasmaclearance(46to87mL/min/kg)andlargesteady-statevolumeofdistribution(3.6to6.8L/kg).Theterminaleliminationhalf-liferangedfrom50to83min.ThegastrointestinalabsorptionfromanaqueoussolutionisveryrapidinmiceandratswithpeakDuP734plasmaconcentrationsattainwithin5and20minfollowingadministration,respectively.Thepeakplasmaconcentrationsindogsandmonkeysareattainedwithin45and130min,respectively.Theabsolutebioavailabilityinmicerangesfrom29to46%atdosesof3.1to30.1mg/kg.Thebioavailabilityincreasesfrom4to10%andfrom14to72%whendosesareincreasedfrom12.5to50mg/kgand1to3mg/kgofDuP734inratsanddogs,respectively.Thebioavailabilityinmonkeysis30.5%at9.3mg/kgDuP734dose.ThedosedependentpharmacokineticsofDuP734isobservedwithinnarrowdoserangesinallanimalspeciesinvestigated[3].REFERENCES[1].LCook,etal.DuP734[1-(cyclopropylmethyl)-4-(2'(4''-fluorophenyl)-2'-Oxoethyl)piperidineHBr],aPotentialAntipsychoticAgent:PreclinicalBehavioralEffects.JPharmacolExpTher.1992Dec;263(3):1159-66.[2].MWatanabe,etal.[H]1-(cyclopropylmethyl)-4-(2-(4-fluorophenyl)-2-oxoethyl)PiperidineHBr(DuP734).ASelectiveLigandforSigmaReceptorsinMouseBraininVivo.JPharmacolExpTher.1993Sep;266(3):1541-8.[3].RPKapil,etal.DoseandSpeciesDependentPharmacokineticsofaNovelSigmaReceptorAntagonist,DuP734.ResCommunMolPatholPharmacol.1995Apr;88(1):3-20.McePdfHeightCaution:Producthasnotb