Pomaglumetad-methionil-hydrochloride-LY2140023-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPomaglumetadmethionilhydrochlorideCat.No.:HY-105040CCASNo.:635318-26-2Synonyms:LY2140023hydrochloride分⼦式:C₁₂H₁₉ClN₂O₇S₂分⼦量:402.87作⽤靶点:mGluR作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:25mg/mL(62.05mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4822mL12.4110mL24.8219mL5mM0.4964mL2.4822mL4.9644mL10mM0.2482mL1.2411mL2.4822mL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(storedundernitrogen)。-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(6.21mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.21mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.21mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pomaglumetadmethionilhydrochloride(LY2140023hydrochloride)⼀种选择性mGlu2/3受体激动剂LY404039的蛋氨酸前药，具有⼝服活性。Pomaglumetadmethionilhydrochloride可⽤于精神分裂症的研究。IC50&TargetmGluR2mGluR3体外研究Pomaglumetadmethionil(LY2140023)isahigh-affinitypeptidetransporter1(PEPT1)substratewithaKmvalueof~30µM[2].LY2140023isactiveagainst[14C]Gly-SarwithanIC50valueof0.018mM[2].体内研究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