Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPW0787Cat.No.:HY-138639CASNo.:2624131-45-7分?式:C??H??F?N?O?分?量:460.42作?靶點:Others作?通路:Others儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據體外實驗DMSO:50mg/mL(108.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1719mL10.8596mL21.7193mL5mM0.4344mL2.1719mL4.3439mL10mM0.2172mL1.0860mL2.1719mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.43mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.43mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性PW0787?種有效的，選擇性的，具有?服活性的，可透過?腦屏障的GPR52激動劑(EC50=135nM)。PW0787抑制精神刺激?為。IC50&TargetEC50:135nM(GPR52)[1]體內研究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:Na?vemaleC57/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