Dorzagliatin-HMS5552-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEDorzagliatinCat.No.:HY-109030CASNo.:1191995-00-2Synonyms:HMS5552分⼦式:C₂₂H₂₇ClN₄O₅分⼦量:462.93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:125mg/mL(270.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1602mL10.8008mL21.6015mL5mM0.4320mL2.1602mL4.3203mL10mM0.2160mL1.0801mL2.1602mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.49mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.49mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoil1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.49mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Dorzagliatin(HMS5552)⼀种双重作⽤的葡萄糖激酶(glucokinase;GK)激活剂，可改2型糖尿病的⾎糖控制和胰腺β细胞功能[1]。IC50&TargetGlucokinase[1]体内研究Dorzagliatin(low-dose10ꢀmg/kg,andhigh-dose30ꢀmg/kg;administeredintragastrically;daily8:00AMforonemonth)exertsaglucose-loweringeffectontheglucoselevelsindiabeticrats[2.AnimalModel:MaleSprague-Dawley(SD)rats(agedapproximately6–8weeksandweighing200-230ꢀg)[2Dosage:Low-dose(10ꢀmg/kg),andhigh-dose(30ꢀmg/kg)Administration:Administeredintragastrically(i.g.);daily(8:00AM)foronemonthResult:Exertedaglucose-loweringeffectontheglucoselevels.REFERENCES[1].ZhuXX,etal.Dorzagliatin(HMS5552),anoveldual-actingglucokinaseactivator,improvesglycaemiccontrolandpancreaticβ-cellfunctioninpatientswithtype2diabetes:A28-daytreatmentstudyusingbiomarker-guidedpatientselection.DiabetesObesMetab.2018Sep;20(9):2113-2120.[2].WangP,etal.EffectsofaNovelGlucokinaseActivator,HMS5552,onGlucoseMetabolisminaRatModelofType2DiabetesMellitus.JDiabetesRes.2017;2017:5812607.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse