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(diǎn):Glucokinase作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥30mg/mL(70.84mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3614mL11.8072mL23.6144mL5mM0.4723mL2.3614mL4.7229mL10mM0.2361mL1.1807mL2.3614mL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(qǐng)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(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.90mM);Clearsolution3.請(qǐng)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(nèi)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