Icosabutate-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIcosabutateCat.No.:HY-121212CASNo.:1253909-57-7分?式:C??H??O?分?量:374.56作?靶點:Others作?通路:Others儲存?式:Pureform-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(266.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6698mL13.3490mL26.6980mL5mM0.5340mL2.6698mL5.3396mL10mM0.2670mL1.3349mL2.6698mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.67mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(6.67mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.67mM);ClearsolutionBIOLOGICALACTIVITY?物活性Icosabutate?種具有?服活性的ω-3多不飽和脂酸，??碳五烯酸的衍?物(EPAderivative)。Icosabutate克服了未經(jīng)修飾的EPA對肝臟靶向的缺點，可改了胰島素敏感性，肝炎和纖維化。Icosabutate具有良好的耐受性，可有效降低持續(xù)性??油三酯?癥中的??密度脂蛋?膽醇(non-HDL-C)?平。IC50&TargetIC50:non-HDL-C[2]體內(nèi)研究Icosabutate(oralgavage;100mg/kg;once)accountsforthemuchhigherflowrateofportalveinplasma(522mL/h)versusmesentericlymph(0.5mL/h),thatdatademonstatethaticosabutateisalmostentirely

takenupthroughtheportalvein(>99%)withonlyasmallfractionoficosabutatebeingabsorbedthroughthelymphaticpathwayin8‐weekoldmaleWistarrats[1].Icosabutate([14‐C]‐icosabutate;oralgavage;100mg/kg;once)

showsthatpeakconcentrationsofradioactivityinmosttissuesat4‐8hoursafterthedose(exceptthegastrointestinal

tract)withhighestconcentrationsintheliverandkidney,mostothertissuescontainlevelsofradioactivitybelowthatin

plasmainmalealbinoWistarrats[1].Icosabutate(dietadministration;135mg/kg/day;5weeks)markedlyimproved

glucosetoleranceafteranoralglucoseload,significantlyreducesAUC(0‐120minutes)by60%withoutaffectingbody

weight,decreaseplasmaalanineaminotransferase(ALT)levelsimprovesglucosemetabolismbyasignificantdecrease

inbloodglucose,bloodhemoglobinA1c,plasmainsulin,andHOMA‐IR(-50%,-47%,-76%and-87%,respectively)in

mice[1].Icosabutate(oraladminstration;112mg/kg/day;20weeks)preventsmicrovesicularsteatosis(-35%)and

hepatocellularhypertrophy(-82%),butnotmacrovesicularsteatosis.After20weeksoftreatment,despitecomparable

decreasesinhepaticinflammatorycellaggregates,onlyicosabutatereducedhepaticcollagencontent[1].AnimalModel:6‐8‐week‐oldmaleob/obmice[1]Dosage:135mg/kgAdministration:135mg/kg/daythroughdietadministration;5weeksResult:Improvedglucosemetabolismandinsulinresistance.AnimalModel:8‐15‐week‐oldmaleAPOE*3Leiden.CETPmicefedahigh‐fatandhighcholesteroldiet[1]Dosage:112mg/kg/dayAdministration:Oralgavage;20weeksResult:Improvedmicrovesicularsteatosis,hepaticinflammation,andfibrosis.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].vandenHoekAM,etal.IcosabutateExertsBeneficialEffectsUponInsulinSensitivity,HepaticInflammation,Lipotoxicity,andFibrosisinMice.HepatolCommun.2019Dec24;4(2):193-207.[2].KasteleinJJ,etal.Icosabutate,aStructurallyEngineeredFattyAcid,ImprovestheCardiovascularRiskProfileinStatin-TreatedPatientswithResidualHypertriglyceridemia.Cardiology.2016;135(1):3-12.McePdfHeightCaution: