TP-024-FTBMT-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETP-024Cat.No.:HY-101787CASNo.:1358575-02-6Synonyms:FTBMT分⼦式:C₁₉H₁₆F₄N₄O分⼦量:392.35作⽤靶点:GPR52作⽤通路:GPCR/GProtein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(127.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5487mL12.7437mL25.4874mL5mM0.5097mL2.5487mL5.0975mL10mM0.2549mL1.2744mL2.5487mL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:≥2.08mg/mL(5.30mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.30mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TP-024(FTBMT)选择性的GPR52激动剂，EC50为75nM[1]。TP-024有抗精神病和促进认知活性[2]。IC50&TargetIC50:75nM(GPR52)[1]体外研究TP-024(FTBMT)(0.1-10μM)increasesintracellularcAMPlevelsinCHOcellsexpressinghuman,mouse,orratGPR52,withpEC50sof7.03,6.85,and6.87,respectively[2].CellViabilityAssay[1]CellLine:CHOcells(expressingGPR52receptors)cAMPassayConcentration:0.1-10μMIncubationTime:30minutesResult:FTBMTactivatedcAMPsignalinginvitro[1].体内研究TP-024(FTBMT)(30mg/kg,90minutes)exhibitsantipsychotic-likeactivitywithoutcausingcatalepsyinmice[2].TP-024(3or10mg/kg,48hours)improvesrecognitionandspatialworkingmemoryinrats[2].TP-024(3,10,30mg/kg,2hours)stimulatesneuronalactivityinbrainregionsrelatedtocognition[2].AnimalModel:MaleLong-Evansrats(9weeksold)[2]Dosage:10mg/kgAdministration:Oral,1hourbeforememorytestResult:A1-hourpretreatmentwithFTBMT(10mg/kg,p.o.)significantlydecreasesthenumberofmemoryerrorsinducedbyMK-801[2].AnimalModel:MaleICRmice(7to8weeksold)[2]Dosage:3–30mg/kgAdministration:Oral,60minutesbefores.c.administrationofMK-801Result:FTBMTincreasesphospho-DARPP32levelsintheNAcslices[2].REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].TokumaruK,etal.Design,synthesis,andpharmacologicalevaluationof4-azolyl-benzamidederivativesasnovelGPR52agonists.BioorgMedChem.2017Jun15;25(12):3098-3115.[2].NishiyamaK,etal.FTBMT,aNovelandSelectiveGPR52Agonist,DemonstratesAntipsychotic-LikeandProcognitiveEffectsinRodents,RevealingaPotentialTherapeuticAgentforSchizophrenia.JPharmacolExpTher.2017Nov;363(2):253-264.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica