AM-2394-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAM-2394Cat.No.:HY-100221CASNo.:1442684-77-6分⼦式:C₂₂H₂₅N₅O₄分⼦量:423.47作⽤靶点:Glucokinase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(70.84mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3614mL11.8072mL23.6144mL5mM0.4723mL2.3614mL4.7229mL10mM0.2361mL1.1807mL2.3614mL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。-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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.90mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.90mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.90mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AM-2394⼀种新型的glucokinase激活剂(GKA)。AM-2394激活葡萄糖激酶(GK)，EC50为60nM。IC50&TargetEC50:60nM(glucokinase)[1]体内研究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