AZD-8529-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAZD-8529Cat.No.:HY-107457CASNo.:1092453-15-0分?式:C??H??F?N?O?分?量:487.47作?靶點(diǎn):mGluR作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:62.5mg/mL(128.21mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0514mL10.2570mL20.5141mL5mM0.4103mL2.0514mL4.1028mL10mM0.2051mL1.0257mL2.0514mL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。-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:≥6.25mg/mL(12.82mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性AZD-8529?種有效的，?度選擇性的，可?服的mGluR2正向調(diào)節(jié)劑，EC50值為285nM；在20-25M的濃度范內(nèi)，對(duì)mGluR1，3，4，5，6，7和8沒(méi)有正向調(diào)節(jié)作?。IC50&TargetmGluR2285nM(EC50)體外研究AZD-8529potentiatestheeffectsofglutamateatmGluR2withanEC50of195nM[1].AZD-8529doesnotelicitantagonistresponsesonmGluRsat25μM[1].體內(nèi)研究AZD-8529(0.3-mg/kg,i.m.)reducesnicotinepriming-inducedandcue-inducedreinstatementinsquirrelmonkeys[1].AZD-8529(30mg/kg;i.p.)decreasestheincreasedextracellulardopamineinducedbynicotineinaccumbensshelloffreely-movingrats[1].AnimalModel:Sprague-Dawleyrats[1]Dosage:10mg/kg,30mg/kgAdministration:Intraperitonealinjection;2hoursbeforenicotineinjectionsResult:Decreasedtheincreasedextracellulardopamineinducedbynicotine(0.4mg/kg,s.c.)inaccumbensshelloffreely-movingrats.REFERENCES[1].JustinovaZ,etal.TheNovelMetabotropicGlutamateReceptor2PositiveAllostericModulator,AZD8529,DecreasesNicotineSelf-AdministrationandRelapseinSquirrelMonkeys.BiolPsychiatry.2015Oct1;78(7):452-62.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te