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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Elafibranor（同义词：GFT505）/HY-16737/100mg
商品详细Medchemexpress/Elafibranor（同义词：GFT505）/HY-16737/100mg
Medchemexpress/Elafibranor（同义词：GFT505）/HY-16737/100mg
Medchemexpress/Elafibranor（同义词：GFT505）/HY-16737/100mg
商品编号： HY-16737-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1580.00
美元价： 948.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
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%