RO0711401-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERO0711401Cat.No.:HY-124419CASNo.:714971-87-6分?式:C??H??F?N?O?分?量:360.29作?靶點:mGluR作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(277.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7755mL13.8777mL27.7554mL5mM0.5551mL2.7755mL5.5511mL10mM0.2776mL1.3878mL2.7755mL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備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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>>90%cornoilSolubility:≥2.5mg/mL(6.94mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性RO0711401?種選擇性的具有?服活性的mGlu1受體的正變構(gòu)調(diào)節(jié)劑，EC50為56nM。IC50&TargetmGluR156nM(EC50)體內(nèi)研究RO0711401(10mg/kg;s.c.;once)causesalong-lastingimprovementinmotorperformance,whichismaintainedtothesameextentatleastfor6days[1].SystemicinjectionofRO0711401isshowntoreducethefrequencyofspike-and-wavedischargesinaratmodelofabsenceepilepsy,andtoimprovemotorsignsinautoimmuneencephalomyelitis(EAE)mice[1].AnimalModel:Spinocerebellarataxiatype1(SCA1)mice(30-weekold)[1]Dosage:10mg/kgAdministration:Subcutaneousinjection;onceResult:Causedaprolongedimprovementofmotorperformanceontherotarodandthepaw-printtests.REFERENCES[1].SerenaNotartomaso,etal.PharmacologicalenhancementofmGlu1metabotropicglutamatereceptorscausesaprolongedsymptomaticbenefitinamousemodelofspinocerebellarataxiatype1.MolBrain.2013Nov19;6:48.[2].EricVieira,etal.Fluorinated9H-xanthene-9-carboxylicacidoxazol-2-yl-amidesaspotent,orallyavailablemGlu1receptorenhancers.BioorgMedChemLett.2009Mar15;19(6):1666-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te