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

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.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(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:125mg/mL(270.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1602mL10.8008mL21.6015mL5mM0.4320mL2.1602mL4.3203mL10mM0.2160mL1.0801mL2.1602mL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:≥2.08mg/mL(4.49mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.49mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥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.DiabetesObes[2].WangP,etal.EffectsofaNovelGlucokinaseActivator,HMS5552,onGlucoseMetabolisminaRatModelofType2DiabetesMellitus.JDiabetesRes.2017;2017:5812607.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu