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蚂蚁淘在线 / 品牌中心 / MCE / Medchemexpress/Elafibranor(Synonyms: GFT505)/HY-16737/10mM*1mL in DMSO

Medchemexpress/Elafibranor(Synonyms: GFT505)/HY-16737/10mM*1mL in DMSO

价格
￥1580.00
货号：HY-16737-10mM*1mLinDMSO
浏览量：84
品牌：MCE
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商品描述
ElafibranorisanagoNISToftheperoxisomeproliferator-activatedreceptor-α(PPAR-α)andperoxisomeproliferator-activatedreceptor-δ(PPAR-δ)withEC50valuesof45and175nM,respectively.
Description

Elafibranorisanagonistoftheperoxisomeproliferator-activatedreceptor-α(PPAR-α)andperoxisomeproliferator-activatedreceptor-δ(PPAR-δ)withEC50valuesof45and175nM,respectively.

IC50&Target

EC50:45nM(PPAR-α),175nM(PPAR-δ)[1]

InVitro

GFT505isbeingdevelopedasadualPPAR-α/PPAR-δagonistforthetreatmentofT2DMandnon-alcoholicfattyliverdisease.GFT505hasanactivemetabolite,GFT1007,andbothhavepotentagonistactivityforPPAR-αandtoalesserextentforPPAR-δ[1].

InVivo

GFT505improvesinsulinsensitivityandearlystudiesindicateitmaybeusefulinnon-alcoholicfattyliverdiseasewhichisbeingtestedinaPhaseIIbstudy[1].Elafibranoriswelltoleratedanddoesnotcauseweightgainorcardiacevents,butdoesproduceamild,reversIBLeincreaseinserumcreatinine.Elafibranorimprovesinsulinsensitivity,glucosehomeostasis,andlipidmetabolismandreducesinflammation[2].GFT505treatmentimprovesglucosecontrolandplasmalipidsindiabeticdb/dbmice.Asignificantdose-dependentreductionofhepaticexpressionofthekeygluconeogenicenzymesglucose6-phosphatase(G6Pase),PEPCK,andfructose1,6-bisphosphatase1(FBP1)isobservedwithGFT505.GFT505doesnotinducecardiacadverseeffectsofPPARγ-activatingagonistsinmonkeys[3].

ClinicalTrial
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References

  • [1].LiuZM,etal.EarlyinvestigationaldrugstargetingPPAR-αforthetreatmentofmetabolicdisease.ExpertOpinInvestigDrugs.2015May;24(5):611-21.

    [2].RatziuV,etal.Elafibranor,anAgonistofthePeroxisomeProliferator-ActivatedReceptor-αand-δ,InducesResolutionofNonalcoholicSteatohepatitisWithoutFibrosisWorsening.Gastroenterology.2016May;150(5):1147-1159.

    [3].HanfR,etal.Thedualperoxisomeproliferator-activatedreceptoralpha/deltaagonistGFT505exertsanti-diabeticeffectsindb/dbmicewithoutperoxisomeproliferator-activatedreceptorgamma-associatedadversecardiaceffects.DiabVascDisRes.2014No

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.6008mL13.0042mL26.0085mL
5mM0.5202mL2.6008mL5.2017mL
10mM0.2601mL1.3004mL2.6008mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
References

  • [1].LiuZM,etal.EarlyinvestigationaldrugstargetingPPAR-αforthetreatmentofmetabolicdisease.ExpertOpinInvestigDrugs.2015May;24(5):611-21.

    [2].RatziuV,etal.Elafibranor,anAgonistofthePeroxisomeProliferator-ActivatedReceptor-αand-δ,InducesResolutionofNonalcoholicSteatohepatitisWithoutFibrosisWorsening.Gastroenterology.2016May;150(5):1147-1159.

    [3].HanfR,etal.Thedualperoxisomeproliferator-activatedreceptoralpha/deltaagonistGFT505exertsanti-diabeticeffectsindb/dbmicewithoutperoxisomeproliferator-activatedreceptorgamma-associatedadversecardiaceffects.DiabVascDisRes.2014No

MolecularWeight

384.49

Formula

C₂₂H₂₄O₄S

CASNo.

923978-27-2

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥33mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.31%