Midaglizole-racemic-DG5128-free-base-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMidaglizoleCat.No.:HY-148529CASNo.:66529-17-7Synonyms:(±)-DG5128freebase;DG5128freebase分⼦式:C₁₆H₁₇N₃分⼦量:251.33作⽤靶点:AdrenergicReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:162.5mg/mL(646.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.9788mL19.8942mL39.7883mL5mM0.7958mL3.9788mL7.9577mL10mM0.3979mL1.9894mL3.9788mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥16.25mg/mL(64.66mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥16.25mg/mL(64.66mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥16.25mg/mL(64.66mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Midaglizole((±)-DG5128freebase,DG5128freebase)⼀种有效的α2-adrenoceptor拮抗剂。Midaglizole⼀种降⾎糖药。Midaglizole在具有升⾼⾎压并降低⾎糖⽔平的作⽤[1][2][3]。体外研究MidaglizolestimulatesinsulinreleasewiththeEC50valuesof200nM,24µMforratisletsandMIN6β-cellline,respectively[3].体内研究Midaglizole(3,30mg/kg;i.v.)increasesbloodpressureinrats[1].Midaglizole(0.2,1,2mg/kg;infusion)reducesbloodglucoselevelsindags[2].AnimalModel:290-450g,MaleWistarrats[1]Dosage:3,30mg/kgAdministration:I.v.Result:Increasedthebloodpressureby27and64mmHgat3,30mg/kg,respectively.AnimalModel:Dogs[2]Dosage:0.2,1,2mg/kgAdministration:SuperiorpancreaticoduodenealarteryinfusionResult:Reducedbloodglucoselevelsbystimulatinginsulinreleasefromthepancreaticislets.REFERENCES[1].HirohashiM,etal.Intrinsicpressoractivityofmidaglizole,analpha-2adrenoceptorantagonist,inpithedrats.JpnJPharmacol.1990Aug;53(4):519-20.[2].OhnedaK,etal.Mechanismofinsulinsecretionbymidaglizole.DiabetesResClinPract.1993Feb;19(2):127-32.[3].ProksP,etal.InhibitionofrecombinantK(ATP)channelsbytheantidiabeticagentsmidaglizole,LY397364andLY389382.EurJPharmacol.2002Sep27;452(1):11-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio