Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETP-024Cat.No.:HY-101787CASNo.:1358575-02-6Synonyms:FTBMT分?式:C??H??F?N?O分?量:392.35作?靶點(diǎn):GPR52作?通路:GPCR/GProtein儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(127.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5487mL12.7437mL25.4874mL5mM0.5097mL2.5487mL5.0975mL10mM0.2549mL1.2744mL2.5487mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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:≥2.08mg/mL(5.30mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.30mM);ClearsolutionBIOLOGICALACTIVITY?物活性TP-024(FTBMT)選擇性的GPR52激動(dòng)劑，EC50為75nM[1]。TP-024有抗精神病和促進(jìn)認(rèn)知活性[2]。IC50&TargetIC50:75nM(GPR52)[1]體外研究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].體內(nèi)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?邊的抑制劑?師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