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Medchemexpress/AVE 0991/HY-15778/10mM*1mL in DMSO

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Medchemexpress/AVE 0991/HY-15778/10mM*1mL in DMSO

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MedChemExpress

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HY-15778-10mM*1mLinDMSO

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AVE0991isanonpeptideandorallyactiveAng-(1-7)agoNIST.AVE0991competesforhigh-affinitybindingof[¹²⁵I]-Ang-(1-7)tobovineaorticendothelialcellmembraneswithIC₅₀of21±35nM.

CustomerValidation

•Diabetes.2017Aug;66(8):2201-2212.
•PLoSOne.2015Nov5;10(11):e0142087.

Description	AVE0991isanonpeptideandorallyactiveAng-(1-7)agonist.AVE0991competesforhigh-affinitybindingof[¹²⁵I]-Ang-(1-7)tobovineaorticendothelialcellmembraneswithIC₅₀of21±35nM.
IC₅₀&Target	IC50:21±35nM(Ang-(1-7)receptor)^[1]
InVitro	AVE0991isanonpeptidecompoundthatevokeseffectssimilartoAng-(1-7)ontheendothelium.AVE0991andunlabeledAng-(1-7)competeforhigh-affinitybindingof[¹²⁵I]-Ang-(1-7)tobovineaorticendothelialcellmembraneswithIC₅₀sof21±35and220±280nM,respectively.PeakconcentrationsofNOandO₂^-releasebyAVE0991sodiumsaltandAng-(1-7)(both10μM)arenotsignificantlydifferent(NO:295±20and270±25nM;O₂^-:18±2and20±4nM).However,thereleasedamountofbioactiveNOis≈5timeshigherforAVE0991incomparisontoAng-(1-7)^[1].
InVivo	AVE0991(0.58nmol/g)producesasignificantdecreaseofwaterdiuresisinWTmicecomparedwithvehicle-treatedanimals(0.06±0.03mLversus0.27±0.05;n=9foreachgroup;P<0.01). the="" antidiuretic="" effect="" of="" ave="" 0991="" (ave)="" is="" associated="" with="" an="" increase="" in="" urine="" osmolality="" (1669±231.0="">₂Oversus681.1±165.8mOsm/KgH₂Oinvehicle-treatedmice;P<0.01). the="" genetic="" deletion="" of="">MasabolishestheantidiureticeffectofAVE0991duringwaterloADIng(0.37±0.10mL[n=9]versus0.27±0.03mL[n=11]inAVE0991-treatedmice).AsobservedwithC57BL/6mice,administrationofAVE0991(0.58nmol/g)inwater-loadedSwissmicealsoproducesasignificantdecreaseoftheurinaryvolumecomparedwithvehicle-treatedanimals(0.13±0.05mL[n=16]versus0.51±0.04mL[n=40];P<>^[2].OneweekoftreatmentwithAVE-0991producesasignificantdecreaseinperfusionpressure(56.55±0.86vs.68.73±0.69mmHginvehicle-treatedrats)andanincreaseinsystolictension(11.40±0.05vs.9.84±0.15ginvehicle-treatedrats),rateoftensionrise(+dT/dt;184.30±0.50vs.155.20±1.97g/sinvehicle-treatedrats),rateoftensionfall(−dT/dt;179.60±1.39vs.150.80±2.42g/sinvehicle-treatedrats).Aslightincreaseinheartrate(HR)isalsoobserved(220.40±0.71vs.214.20±0.74beats/mininvehicle-treatedrats^[3].
References	[1].WiemerG,etal.AVE0991,anonpeptidemimicoftheeffectsofangiotensin-(1-7)ontheendothelium.Hypertension.2002Dec;40(6):847-52. [2].PinheiroSV,etal.NonpeptideAVE0991isanangiotensin-(1-7)receptorMasagonistinthemousekidney.Hypertension.2004Oct;44(4):490-6. [3].FerreiraAJ,etal.Thenonpeptideangiotensin-(1-7)receptorMasagonistAVE-0991attenuatesheartfailureinducedbymyocardialinfarction.AmJPhysiolHeartCircPhysiol.2007Feb;292(2):H1113-9.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	1.7220mL	8.6100mL	17.2200mL
5mM	0.3444mL	1.7220mL	3.4440mL
10mM	0.1722mL	0.8610mL	1.7220mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

KinaseAssay
^[1]

Bindingof[¹²⁵I]-Ang-(1-7)isperformed.Briefly,100μgofmembranesfromprimaryculturedbovineaorticendothelialcells(BAECs,passage1)areincubatedinatotalvolumeof200μLfor45minutesat25°CinHEPES-bufferedsaline(10mMHEPES,0.1MNaCl,5mMMgCl₂)containing0.2%BSAandproteaseinhibitorcocktailComplete(BoehringerMannheim).Saturablebindingof[¹²⁵I]-Ang-(1-7)iscalculatedbysubtractingnonspecificbinding(40%to50%),determinedinthepresenceof10μMunlabeledAng-(1-7)fromtotalbinding.CompetitionexperimentswithincreasingconcentrationsofAVE0991andunlabeledAng-(1-7)areperformedinthepresenceof10nM[¹²⁵I]-Ang-(1-7).Assaysareterminatedbyvacuumfiltration(≤15mmHg)overDuraporefilters(0.65μm,Opak96-wellplates)presoakedwith1%BSA.Thefiltersarewashed3timeswitheach100μLofPBS(50mM,NaHPO₄and0.15MNaCl,pH7.2).Radioactivityondriedfiltersisquantifiedwithagammacounter^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
^[1]

Monkeykidney(COS)cellsandChinesehamsterovary(CHO)cellsarestablytransfectedwithrat Mas CDNAdrivenbyacytomegaloviruspromoterandselectedbyneomycin.¹²⁵I-Ang-(1-7)(0.5×10^-9 mol/L)isincubatedin24-wellplatesfor60minutesat4°Cin0.3mLofserum-freemedium(DMEM)supplementedwith0.2%BSA,0.005%bacitracin,0.1mol/LPMSF,and0.5mol/Lorthophenanthrolinewith Mas-transfectedCOScellsinthepresenceorabsenceofAVE0991(AVE,10^-10 to^-5 mol/L).After2isheswithice-coldserum-freeDMEM,cellsaredisruptedwith0.1%TritonX-100.Boundradioactivityismeasuredinagammacounter.Bindingofrhodamine-Ang-(1-7)in Mas-transfectedCHOcellsisperformedundersimilarconditionsusing2×10^-9 mol/Lrhodamine-labeled-Ang-(1-7)inthepresenceorabsenceofAVE(10^-6 mol/L),CV11974(10^-6 mol/L),orPD123319(10^-6 mol/L).NSBisdeterminedinthepresenceof10^-6mol/LAng-(1-7)^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
^[2]^[3]

AVE0991(AVE)ispreparedin10μMKOH(Mice)^[2].
AVE0991ispreparedin0.9%NaCl(Rat)^[3].

Mice^[2]
Swissmalemice,Mas-KO(Mas^-/-)malemiceonthepuregeneticbackgroundC57BL/6,andWTC57BL/6controlmice(Mas^+/+)areused.Waterdiuresisisinducedbyintraperitonealwaterinjection(0.05mL/gofbodyweight[BW])inconsciousmice.Drugsareadministeredinthesameinjectionwithwaterloadatprefixedvolumes(0.01mL/gBW).Inthefirstsetofexperiments,WTmice(C57BL/6,controlgroup)orMas-KOmicearetreatedwith:(1)0.58nmol/gAVE0991(n=9,control;n=11,Mas-KOmice);or(2)vehicleforAVE0991(10μMKOH,0.01mL/g;n=9,control;n=9,Mas-KO).Inthesecondset,Swissmicearetreatedwith:(1)vehicle(n=36);(2)0.58nmol/gAVE0991(n=16);(3)46pmol/gAng-(1-7)antagonistA-779(n=4);(4)2nmol/glosartanorvalsartan(n=5);(5)2nmol/gAT₂receptorantagonistsPD123319orPD123177(n=9);(6)AVE0991combinedwithA-779;(7)AVE0991combinedwithlosartanorvalsartan(n=4foreach);(8)orAVE0991combinedwithPD123319(n=5)orPD123177(n=4).Theurinaryvolumeismeasuredfor60minutesafterwaterloading,andurinesamplesareobtainedtodeterminetheosmolality.ThedoseofAVE0991isbasedinpreliminaryexperimentsperformedinSwissmice.
Rat^[3]
MaleWistarratsweighting250-300gareused.RatsaretreatedeitherwithAVE-0991(1mg/kg,n=9)orvehicle(0.9%NaCl,n=11)administeredorallybygavage.Attheendofthe7dayperiodofAVE-0991treatment,theanimalsaredecapitated10-15minafterintraperitonealinjectionof400IUofheparin.Afterthethoraxisopened,theheartiscarefullydissected,removedfromthethoraciccavity,andplacedinaplatecontainingice-coldKrebs-Ringersolution(KRS)toattenuateanypotentialcardiacdamageduringdissectionofaortaartery.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].WiemerG,etal.AVE0991,anonpeptidemimicoftheeffectsofangiotensin-(1-7)ontheendothelium.Hypertension.2002Dec;40(6):847-52.
[2].PinheiroSV,etal.NonpeptideAVE0991isanangiotensin-(1-7)receptorMasagonistinthemousekidney.Hypertension.2004Oct;44(4):490-6.
[3].FerreiraAJ,etal.Thenonpeptideangiotensin-(1-7)receptorMasagonistAVE-0991attenuatesheartfailureinducedbymyocardialinfarction.AmJPhysiolHeartCircPhysiol.2007Feb;292(2):H1113-9.

MolecularWeight

580.72

Formula

C₂₉H₃₂N₄O₅S₂

CASNo.

304462-19-9

Storage

Powder	-20°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO

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

Purity:99.16%

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