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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/INT-777（同义词：S-EMCA）/HY-15677/10mg
商品详细Medchemexpress/INT-777（同义词：S-EMCA）/HY-15677/10mg
Medchemexpress/INT-777（同义词：S-EMCA）/HY-15677/10mg
Medchemexpress/INT-777（同义词：S-EMCA）/HY-15677/10mg
商品编号： HY-15677-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥9240.00
美元价： 5544.00
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
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商品介绍
INT-777isapotentTGR5agoNISTwithEC50of0.82μM.

CustomerValidation

  • •Immunity.2016Oct18;45(4):944.
  • •Oncotarget.2017Apr29;8(33):54378-54387.
  • •Endocrine.2016Dec;54(3):657-670.
  • •ChineseJournalofPathophysiology.2017,33(2):239-243.
Description

INT-777isapotentTGR5agonistwithEC50of0.82μM.

IC50&Target

EC50:0.82μM(TGR5)

InVitro

INT-777isanovelpotentandselectiveTGR5agonistwithremarkableinvivoactivity[1].INT-777(3μM)increasesATPproductioninthehumanenteroendocrinecelllineNCI-H716inacAMP-dependentmanner[2].INT-777(10μM)lowersIscandincreasesTEERwhenaddedontheSEROsalsideofseromuscularstrippeddistalcolonsegments.INT-777effectonbasalsecretionisreducedinneuron-freeandTTX-treatedmucosal-submucosalpreparations[3].

InVivo

INT-777(30mg/kg/day,p.o.)increasesenergyexpenditureandreduceshepaticsteatosisandobesityuponhighfatfeeding,andimprovesinsulinsensitivity,inTGR5-Tgmice[2].INT-777(1μM/min/kg,p.o.)hasapotentcholereticeffect,preventscarboxylCoAactivationandsubsequentconjugation,therebyfavoringitscholehepaticshuntpathwaywithaductularabsorptionandapotentcholereticeffectinHF-fedTGR5-Tgmalemice[4].

References

  • [1].PellicciariR,etal.Discoveryof6alpha-ethyl-23(S)-methylcholicacid(S-EMCA,INT-777)asapotentandselectiveagonistfortheTGR5receptor,anoveltargetfordiabesity.JMedChem.2009Dec24;52(24):7958-61.

    [2].ThomasC,etal.TGR5-mediatedbileacidsensingcontrolsglucosehomeostasis.CellMetab.2009Sep;10(3):167-77.

    [3].DubocH,etal.ReductionofepithelialsecretioninmaleratdistalcolonicmucosabybileacidreceptorTGR5agonist,INT-777:roleofsubmucosalneurons.NeurogastroenterolMotil.2016Jun3.doi:10.1111/nmo.

    [4].PellicciariR,etal.Discoveryof6alpha-ethyl-23(S)-methylcholicacid(S-EMCA,INT-777)asapotentandselectiveagonistfortheTGR5receptor,anoveltargetfordiabesity.Format:AbstractSendtoJMedChem.2009Dec24;52(24):7958-61.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.2190mL11.0951mL22.1902mL
5mM0.4438mL2.2190mL4.4380mL
10mM0.2219mL1.1095mL2.2190mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

INT-777isdissolvedinDMSO.

TheexperimentsarecarriedoutinSTC-1orNCI-H716cellstreatedwithvehicle(DMSO)orINT-777.INT-777isassessedforitsagonisticactivityonTGR5.cAMPproductionisperformed.CytochromeCoxidaseactivityisevaluatedbyfollowingtheoxidationoffullyreducedcytochromeCat550nm.ATP/ADPratioandGLP-1releaseismeasuredaccordingtothemanufacturer"sinstruction.PrimarybrownADIpocytesarepreparedandilealexplantsareprepared.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2]

INT-777ismixedwithdiet.

Age-matchedmalemiceareusedforallexperiments.Geneticallyengineeredmousemodels(GEMMs),i.e.TGR5-TgandTGR5-/-micearegenerated.Diet-inducedobesity(DIO)intheGEMMsorC57BL/6Jmiceisinducedbyfeeding8-week-oldmicewithaHF-diet(60%Cal/fat,D12492)foratleast8weeks,asmentionedinthetextandfigurelegends.Inthedietaryinterventionexperiments,INT-777ismixedwithdietatthedosesufficienttoreachaninvivodoseof30mg/kg/d.MousephenotypingexperimentsareperformedaccordingtoEMPRESSprotocolsandaimedtoassessfoodandwaterintake,bodycomposition,energyexpenditure,glucoseandlipidhomeostasis,andplasmabiochemistry.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].PellicciariR,etal.Discoveryof6alpha-ethyl-23(S)-methylcholicacid(S-EMCA,INT-777)asapotentandselectiveagonistfortheTGR5receptor,anoveltargetfordiabesity.JMedChem.2009Dec24;52(24):7958-61.

    [2].ThomasC,etal.TGR5-mediatedbileacidsensingcontrolsglucosehomeostasis.CellMetab.2009Sep;10(3):167-77.

    [3].DubocH,etal.ReductionofepithelialsecretioninmaleratdistalcolonicmucosabybileacidreceptorTGR5agonist,INT-777:roleofsubmucosalneurons.NeurogastroenterolMotil.2016Jun3.doi:10.1111/nmo.

    [4].PellicciariR,etal.Discoveryof6alpha-ethyl-23(S)-methylcholicacid(S-EMCA,INT-777)asapotentandselectiveagonistfortheTGR5receptor,anoveltargetfordiabesity.Format:AbstractSendtoJMedChem.2009Dec24;52(24):7958-61.

MolecularWeight

450.65

Formula

C₂₇H₄₆O₅

CASNo.

1199796-29-6

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥31mg/mL

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

Purity:>98.0%