PW0787-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPW0787Cat.No.:HY-138639CASNo.:2624131-45-7分⼦式:C₂₃H₂₀F₄N₄O₂分⼦量:460.42作⽤靶点:Others作⽤通路:Others储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:50mg/mL(108.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1719mL10.8596mL21.7193mL5mM0.4344mL2.1719mL4.3439mL10mM0.2172mL1.0860mL2.1719mL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(protectfromlight)。-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:≥2.5mg/mL(5.43mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.43mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性PW0787⼀种有效的，选择性的，具有⼝服活性的，可透过⾎脑屏障的GPR52激动剂(EC50=135nM)。PW0787抑制精神刺激⾏为。IC50&TargetEC50:135nM(GPR52)[1]体内研究PW0787(0.3,1,3,or10mg/kg;IP)displaysantipsychotic-likeactivitybysignificantlyinhibitingamphetamine-inducedhyperlocomotorbehaviorinmice[1].PW0787isevaluatedinratsafterasingledoseof20mg/kgbyoral(PO)or10mg/kgbyintravenous(IV)administration.PW0787hasexcellentplasmaexposureafterPO(AUC0-inf=13,749ng•h/mL)andIVdosing(AUC0-inf=9030ng•h/mL),aswellashighmaximumserumconcentrationfollowingPO(Cmax=3407ng/mL)andIVadministration(Cmax=6726ng/mL).Additionally,PW0787displaysgoodvolumeofplasmadistribution(Vss=1.5L/kg)andacceptableplasmaclearance(CL=1.1L/h/kg)after10mg/kgIV.Excellentoralbioavailability(F)withthevalueof76%isobserved[1].AnimalModel:NaïvemaleC57/BL6miceweighingbetween24and31gDosage:0.3,1,3,or10mg/kg(dissolvedin0.9%salinecontaining20%HP-β-CDwithafinalpHofthesolutionadjustedto7.4)Administration:IPResult:Suppressedamphetamine(AMPH)-inducedhorizontalactivityatboth3mg/kgand10mg/kgdoses.REFERENCES[1].WangP,etal.DiscoveryofPotentandBrain-PenetrantGPR52AgonistthatSuppressesPsychostimulantBehavior.JMedChem.2020;63(22):13951-13972.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forres