Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPomaglumetadmethionilhydrochlorideCat.No.:HY-105040CCASNo.:635318-26-2Synonyms:LY2140023hydrochloride分?式:C??H??ClN?O?S?分?量:402.87作?靶點(diǎn):mGluR作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(62.05mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4822mL12.4110mL24.8219mL5mM0.4964mL2.4822mL4.9644mL10mM0.2482mL1.2411mL2.4822mL請(qǐng)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(qǐng)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(storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.21mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.21mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.21mM);ClearsolutionBIOLOGICALACTIVITY?物活性Pomaglumetadmethionilhydrochloride(LY2140023hydrochloride)?種選擇性mGlu2/3受體激動(dòng)劑LY404039的蛋氨酸前藥，具有?服活性。Pomaglumetadmethionilhydrochloride可?于精神分裂癥的研究。IC50&TargetmGluR2mGluR3體外研究Pomaglumetadmethionil(LY2140023)isahigh-affinitypeptidetransporter1(PEPT1)substratewithaKmvalueof~30μM[2].LY2140023isactiveagainst[14C]Gly-SarwithanIC50valueof0.018mM[2].體內(nèi)研究Pomaglumetadmethionil(LY2140023;orally;3-300mg/kg;oncedailyfor7days)dose-dependentincreasesthelevelsofthedopaminemetabolitesdihydroxyphenylaceticacid(DOPAC)andhomovanillicacid(HVA)[1].AnimalModel:MaleFischerrats(approximately250g)[1]Dosage:3mg/kg,10mg/kg,and300mg/kgAdministration:Orally;oncedailyfor7daysResult:Dose-dependentincreasedthelevelsofthedopaminemetabolitesDOPACandHVA.REFERENCES[1].LoweS,etal.EffectsofanovelmGlureceptoragonistprodrug,LY2140023monohydrate,oncentralmonoamineturnoverasdeterminedinhumanandratcerebrospinalfluid.Psychopharmacology(Berl).2012Feb;219(4):959-70.[2].YAnnePak,etal.InVitroandClinicalEvaluationsoftheDrug-DrugInteractionPotentialofaMetabotropicGlutamate2/3ReceptorAgonistProdrugwithIntestinalPeptideTransporter1.DrugMetabDispos.2017Feb;45(2):137-144.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio