Orforglipron-hemicalcium-hydrate-LY3502970-hemicalcium-hydrate-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEOrforglipronhemicalciumhydrateCat.No.:HY-112185ACASNo.:3008544-96-2Synonyms:LY3502970hemicalciumhydrate;GLP-1receptoragonist1hemicalciumhydrate分子式:C₄₈H₄₈F₂N₁₀O₅.₁/₂Ca.H₂O分子量:921.02作用靶点:GCGR作用通路:GPCR/GProtein储存方式: 4°C,sealedstorage,awayfrommoistureInsolvent:-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)溶解性数据体外实验DMSO:25mg/mL(27.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.0858mL5.4288mL10.8575mL5mM0.2172mL1.0858mL2.1715mL10mM0.1086mL0.5429mL1.0858mL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。BIOLOGICALACTIVITY生物活性Orforglipronhemicalciumhydrate(LY3502970hemicalciumhydrate;GLP-1receptoragonist1hemicalciumhydrate)是Orforglipron(HY-112185)的钙盐水合物形式。Orforglipronhemicalciumhydrate是一种口服有效的胰高血糖素样肽-1受体(GLP-1R)激动剂，可改善2型糖尿病[1]。1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE体内研究Orforglipronhemicalciumhydrate(0.94-4.8nMinplasmaconcentration,i.v.,or0.05-0.1mg/mL,i.g.for5days)suppressesfoodintakeinadose-dependentmanner,promotesinsulinsecretionandbloodglucosereductionincynomolgusmonkeymodel[1].Orforglipronhemicalciumhydrate(0.05-1.35mg/kg,i.g.)reachesCmax2hoursafteradministrationatalldoses,exhibitsproportionalratioofincreaseinplasmadrugexposuretodoseincrease,indicatesadose-dependentabsorptioninthegastrointestinaltract[1].PharmacokineticAnalysisofOrforglipronhemicalciumhydrateincynomolgusmonkey[1]routeDose(mg/kg)Tmax(h)Cmax(ng/mL)AUC0-24h(ng·h/mL)i.g.0.052.04.7823.7i.g.0.152.020.7135i.g.0.452.032.0208i.g.1.352.01481040AnimalModel:cynomolgusmonkeymodel[1]Dosage:0.9-4.8nM;or0.05-0.1mg/mLAdministration:continuousi.v.administrationfor30minutesuntilaplasmaconcentrationof0.9-4.8nMatsteadystate;i.g.for5dayswithdoseof0.05-0.1mg/mLResult:Increasedinsulinsecretionanddecreasedplasma-glucose.Suppressedfoodintakeinadose-dependentmanner.REFERENCES[1].Pyrazolopyridinederivativehavingglp-1receptoragonisteffect.WO2018056453A1McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu