DSR-141562-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEDSR-141562Cat.No.:HY-136569CASNo.:2007975-22-4分⼦式:C₁₉H₂₅F₃N₄O₃分⼦量:414.42作⽤靶点:Phosphodiesterase(PDE)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(120.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4130mL12.0651mL24.1301mL5mM0.4826mL2.4130mL4.8260mL10mM0.2413mL1.2065mL2.4130mL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:≥2.5mg/mL(6.03mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.03mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.03mM);Clearsolution1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性DSR-141562⼀种新型的，具有⼝服活性的、可通透⾎脑屏障的磷酸⼆酯酶(PDE)抑制剂。DSR-141562对⼈PDE1B具有优先选择性，IC50为43.9nM，⼈PDE1A和1C的IC50值分别为97.6nM和431.8nM。DSR-141562⽤于精神分裂症相关症状及认知障碍的相关研究。IC50&TargetIC50:43.9nM(humanPDE1B)IC50:97.6nM(humanPDE1A)IC50:431.8nM(humanPDE1C)体内研究DSR-141562(oraladministration;30mg/kg;singledose;plasmaandbrainexposures0.5,1,2,and3hoursafteradministration)exhibitsgoodbrainuptake,withthebrain-to-bloodconcentrationratioofunbounddrugbeing0.99inrats.DSR-141562(oraladministration;10mg/kg;singledose;2hours)slightlybutsignificantlyincreasescGMPcontentsinthefrontalcortexandstriatuminrat[1].DSR-141562(oraladministration;30mg/kgor100mg/kg;singledose;2hours)causesasignificantincreaseincGMPconcentrationinmonkeyCSF.Theplasmaconcentrationsofunboundthiscompoundareabove43.9nM(IC50s)forPDE1Binvitro(43.9nM).DSR-141562causesasignificantincreaseincGMPconcentrationinmonkeyCSF[1].DSR-141562(oraladministration;3mg/kg,10mg/kgand30mg/kg;singledose)significantlyreversesmethamphetamine-inducedlocomotorhyperactivity,buthasnoeffectonspontaneouslocomotoractivityat3and10mg/kg[1].DSR-141562(oraladministration;0.3mg/kg,1mg/kgor3mg/kg)significantlyreversedthephencyclidine-induceddecreaseofsocialinteractiontimeinmice[1].AnimalModel:MaleSpragueDawleyrats[1]Dosage:3mg/kg,10mg/kgand30mg/kgAdministration:Oraladministration;singledoseResult:Inhibitedmethamphetamine-inducedlocomotorhyperactivityinrats,whileithadonlyminimaleffectsonthespontaneouslocomotoractivity.AnimalModel:MaleSpragueDawleyrats[1]Dosage:0.3mg/kg,1mg/kgor3mg/kgAdministration:Oraladministration;singledoseResult:Reversedsocialinteraction.REFERENCES[1].TakeshiEnomoto,etal.ANovelPhosphodiesterase1InhibitorDSR-141562ExhibitsEfficaciesinAnimalModelsforPositive,Negative,andCognitiveSymptomsAssociatedWithSchizophrenia.JPharmacolExpTher[2].TakeshiEnomoto,etal.ThePreclinicalProfileofDSR-141562:ANovelPhosphodiesterase1InhibitorfortheTreatmentofPositiveSymptoms,NegativeSymptomsandCognitiveImpairmentsAssociatedwithSchizophrenia.ProceedingsforThe93rdAnnualMeetingoftheJapanesePharmacologicalSociety2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasno