Dorzagliatin-HMS5552-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEDorzagliatinCat.No.:HY-109030CASNo.:1191995-00-2Synonyms:HMS5552分?式:C??H??ClN?O?分?量:462.93作?靶點(diǎn):Glucokinase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(270.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1602mL10.8008mL21.6015mL5mM0.4320mL2.1602mL4.3203mL10mM0.2160mL1.0801mL2.1602mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.49mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.49mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.49mM);ClearsolutionBIOLOGICALACTIVITY?物活性Dorzagliatin(HMS5552)?種雙重作?的葡萄糖激酶(glucokinase;GK)激活劑，可改2型糖尿病的?糖控制和胰腺β細(xì)胞功能[1]。IC50&TargetGlucokinase[1]體內(nèi)研究Dorzagliatin(low-dose10?mg/kg,andhigh-dose30?mg/kg;administeredintragastrically;daily8:00AMforonemonth)exertsaglucose-loweringeffectontheglucoselevelsindiabeticrats[2.AnimalModel:MaleSprague-Dawley(SD)rats(agedapproximately6–8weeksandweighing200-230?g)[2Dosage:Low-dose(10?mg/kg),andhigh-dose(30?mg/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