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Medchemexpress/GW-1100/HY-50691/10mM*1mL in DMSO
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Medchemexpress/GW-1100/HY-50691/10mM*1mL in DMSO
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HY-50691-10mM*1mLinDMSO
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GW-1100isaselectiveGPR40antagoNISTwithapIC50of6.9.GW1100actsasaGPR40inverseagonist.

CustomerValidation

  • •SciRep.2017Jun28;7(1):4351.
  • •AmJPathol.2015Jan;185(1):185-96.
Description

GW-1100isaselectiveGPR40antagonistwithapIC50of6.9.GW1100actsasaGPR40inverseagonist.

IC50&Target

pIC50:6.9(GPR40)[1]

InVitro

GW-1100(GW1100)dosedependentlyinhibitsGPR40-mediatedCa2+elevationsstimulatedbyGW9508andlinoleicacid(pIC50valuesof5.99±0.03and5.99±0.06,respectively).GW-1100ataconcentrationof1μMproducesasignificantrightwardshiftintheconcentration-responsecurvetoGW9508(pEC50=7.17±0.08intheabsenceandpEC50=6.79±0.09inthepresenceof1μMGW-1100;P<0.05; n="3)." at="" concentrations="" of="" gw-1100="" of="" 3="" μm="" and="" higher="" a="" significant="" decrease="" in="" the="" maximal="" response="" is="" observed="" with="" a="" continuing="" rightward="" shift="" in="" the="">50response[2].GW-1100(GW1100)reducesFFAR1ligand-inducedintracellularcalciuminCHO-K1/bFFAR1cellsandneutrophils.CHO-K1/bFFAR1cellsareincubatedfor15minwith10μMGW1100orvehicle(0.1%DMSO)andthenstimulatedwithvehicle,oleicacid,linoleicacidorGW9508.GW-1100significantlyreducestheincreaseinintracellularcalciuminducedby300μMoleicacid(AUC(60-150s),p<0.05), 100="" μm="" linoleic="" acid="">(60-150s),p<0.05) and="" 10="" μm="" gw9508="">(60-150s),p<>[3].

InVivo

TheintracerebroventricularinjectionofDHA(50µg)andGW9508(1.0µg),aGPR40-selectiveagonist,significantlyreducesmechanicalallodyniaandthermalhyperalgesiaatday7,butnotatday1,afterCFAinjection.TheseeffectsareinhibitedbyintracerebroventricularpretreatmentwithGW-1100(10µg),aGPR40antagonist[4].

References

  • [1].StoddartLA,etal.UncoveringthepharmacologyoftheGprotein-coupledreceptorGPR40:highapparentconstitutiveactivityinguanosine5"-O-(3-[35S]thio)triphosphatebindingstudiesreflectsbindingofanendogenousagonist.MolPharmacol.2007Apr;71(

    [2].BriscoeCP,etal.PharmacologicalregulationofinsulinsecretioninMIN6cellsthroughthefattyacidreceptorGPR40:identificationofagonistandantagonistsmallmolecules.BrJPharmacol.2006Jul;148(5):619-28.

    [3].ManosalvaC,etal.Cloning,identificationandfunctionalcharacterizationofbovinefreefattyacidreceptor-1(FFAR1/GPR40)inneutrophils.PLoSOne.2015Mar19;10(3):e0119715.

    [4].NakamotoK,etal.HypothalamicGPR40signalingactivatedbyfreelongchainfattyacidssuppressesCFA-inducedinflammatorychronicpain.PLoSOne.2013Dec12;8(12):e81563.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.9209mL9.6047mL19.2093mL
5mM0.3842mL1.9209mL3.8419mL
10mM0.1921mL0.9605mL1.9209mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

GW-1100(GW1100)ispreparedinDMSOandstored,andthendilutedwithappropriatemedium(DMSO0.1%)beforeuse[3].

CHO-K1/bFFAR1orCHO-K1/pCDNA3.1cells(2×106cells/2mL)areloadedwith2.5μMFura-2AMfluorescentindicatordyeinrecordingbuffer(10mMHEPES,140mMNaCl,2mMCaCl2,21mMMgCl2,25mMKCl,10mMglucose,pH7.4)for30min,washedthreetimeswithrecordingbuffer,andreturnedtotheincubatorfor10min.Cellsareincubatedwithdifferentconcentrationsofpropionicacid(1,10and30mM),oleicacid(0-500μM),linoleicacid(0-200μM),GW9508(0-100μM),ionomycin(2μM),thapsigargin(2μM)orvehicle(0.1%DMSO).Thefattyacidconcentrationsusedinallexperimentsareintherangeofconcentrationsofhealthyandperipartumcows.Inanothersetofexperiments,cellsareincubatedwitheither10μMGW-1100for15min,2μMU73122for3minorvehicle(0.1%DMSO)for15minandthenstimulatedwitheither300μMoleicacid,100μMlinoleicacidor10μMGW9508.Cellularfluorescence(Ca2+)ismeasuredat509nmemissionwith340/380nmdualwavelengthexcitationusingaLS55spectrofluorimeter.Cuvettetemperaturesaremaintainedat37°Cwithconstantstirring[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[4]

GW-1100(GW1100)ispreparedinDMSOanddilutedwithsalineorPBS[4].

Mice[4]
MaleddYmice(age,4weeks)arehousedincagesat23-24°Cwitha12-hlight-darkcycle(lightsfrom8amto8pm)andfoodandwateradlibitum.DHA(50µg/mouse),theselectiveGPR40-agonistGW9508(1.0-25µg/mouse)andtheGPR40antagonistGW1100(1-10µg/mouse)aredissolvedin1%DMSOandthesolutionisdilutedwithsalinebeforevonFreytesting(1%DMSOfinalconcentration).ThedosesofGW9508arechosenbaseduponourpreviouspublication,whereasGW-1100isselectedonthebasisofpreviousreportsandourpreliminaryexperiments.Underanon-anesthetizedstate,DHAandGW9508areadministeredviatheintracerebroventricular(i.c.v.)route10minbeforeCFAinjection,andGW1100isadministeredviathei.c.v.route10minbeforeGW9508injection.Flavopiridol(5and15nmol/mouse),acyclin-dependentkinaseinhibitor,isadministeredbyi.c.v.injectionintotheleftlateralventricleofthemicetwiceaday(at9:00and19:00)afterCFAtreatment.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].StoddartLA,etal.UncoveringthepharmacologyoftheGprotein-coupledreceptorGPR40:highapparentconstitutiveactivityinguanosine5"-O-(3-[35S]thio)triphosphatebindingstudiesreflectsbindingofanendogenousagonist.MolPharmacol.2007Apr;71(

    [2].BriscoeCP,etal.PharmacologicalregulationofinsulinsecretioninMIN6cellsthroughthefattyacidreceptorGPR40:identificationofagonistandantagonistsmallmolecules.BrJPharmacol.2006Jul;148(5):619-28.

    [3].ManosalvaC,etal.Cloning,identificationandfunctionalcharacterizationofbovinefreefattyacidreceptor-1(FFAR1/GPR40)inneutrophils.PLoSOne.2015Mar19;10(3):e0119715.

    [4].NakamotoK,etal.HypothalamicGPR40signalingactivatedbyfreelongchainfattyacidssuppressesCFA-inducedinflammatorychronicpain.PLoSOne.2013Dec12;8(12):e81563.

MolecularWeight

520.58

Formula

C₂₇H₂₅FN₄O₄S

CASNo.

306974-70-9

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:95.13%

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