Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAM-2394Cat.No.:HY-100221CASNo.:1442684-77-6分?式:C??H??N?O?分?量:423.47作?靶點:Glucokinase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:≥30mg/mL(70.84mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3614mL11.8072mL23.6144mL5mM0.4723mL2.3614mL4.7229mL10mM0.2361mL1.1807mL2.3614mL請根據產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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.90mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.90mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.90mM);ClearsolutionBIOLOGICALACTIVITY?物活性AM-2394?種新型的glucokinase激活劑(GKA)。AM-2394激活葡萄糖激酶(GK)，EC50為60nM。IC50&TargetEC50:60nM(glucokinase)[1]體內研究AM-2394,astructurallydistinctglucokinaseactivatorthatdisplaysarobustreductioninplasmaglucoseduringanoralglucosetolerancetest(OGTT)inob/obmiceatadoseof3mg/kg.AM-2394increasestheaffinityofglucokinase(GK)forglucosebyapproximately10-fold,exhibitsmoderateclearanceandgoodoralbioavailabilityinmultipleanimalmodels,andlowersglucoseexcursionfollowinganoralglucosetolerancetestinanob/obmousemodelofdiabetes.AM-2394exhibitsgood-to-moderatecrossspeciesplasmaclearance,volumeofdistribution,andoralbioavailability,allowingforfurtherevaluationinanimalmodels[1].PROTOCOLAnimalMice[1]Administration[1]InordertodeterminetheeffectofAM-2394inananimalmodeloftype2diabetes,itwasadministeredperos(PO)tomaleob/obmice30minutespriortoperforminganoralglucosetolerancetest(OGTT).Dosesof1,3,10,30mg/kgeachreducedglucoseexcursion,withmaximalefficacyseenat3mg/kg.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].DransfieldPJ,etal.NovelSeriesofPotentGlucokinaseActivatorsLeadingtotheDiscoveryofAM-2394.ACSMedChemLett.2016May23;7(7):714-8.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications