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Medchemexpress/AR-C155858/HY-13248/10mg

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MedChemExpress

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HY-13248-10mM*1mLinDMSO

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4000-520-616

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AR-C155858isanovelinhibitorofthemonocarboxylatetransporters(MCTs)MCT1andMCT2(K_ivaluesare2.3and< 10 nM, respectively), and exhibits no activity at MCT4.

CustomerValidation

•ProcNatlAcadSciUSA.2015Sep1;112(35):11090-5.
•Elife.2017Apr17;6.pii:e24241.
•JNeurosci.2015Mar11;35(10):4168-78.
•Oncotarget.2014Nov30;5(22):11029-37.
•PharmRes.2015Jun;32(6):1894-906.
•JCellPhysiol.2017Jan;232(1):136-44.

•AmJPhysiolCellPhysiol.2016Jul1;311(1):C116-26.
•PLoSOne.2016Apr7;11(4):e0153135.
•PLoSOne.2014Jan21;9(1):e85780.
•PLoSOne.2013;8(2):e57712.
•JPharmPharmacol.2014Apr;66(4):574-83.

Description	AR-C155858isanovelinhibitorofthemonocarboxylatetransporters(MCTs)MCT1andMCT2(K_ivaluesare2.3and<10=""nm,=""respectively),=""and=""exhibits=""no=""activity=""at=""mct4.="">
IC₅₀&Target	Ki:2.3nM(MCT1),10nM(MCT2)
InVitro	AR-C155858(10nM-100nM)inhibitsMCT1/MCT2C-terminalchimaeras^[1].AR-C155858inhibitsMCT2,andthe70%inhibitionseenat10nMisfollowedbyagraduallyincreasinginhibitionwhichcanonlybeexplainedbyaK_ivalueofsignificantlylessthan10nM.AR-C155858inhibitsMCT1expressedinXenopusoocytesinatime-andconcentration-dependentmanner^[2].
References	[1].OvensMJ,etal.Theinhibitionofmonocarboxylatetransporter2(MCT2)byAR-C155858ismodulatedbytheassociatedancillaryprotein.BiochemJ.2010Oct15;431(2):217-25. [2].OvensMJ,etal.AR-C155858isapotentinhibitorofmonocarboxylatetransportersMCT1andMCT2thatbindstoanintracellularsiteinvolvingtransmembranehelices7-10.BiochemJ.2010Jan15;425(3):523-30. [3].VijayN,etal.ANovelMonocarboxylateTransporterInhibitorasaPotentialTreatmentStrategyforγ-HydroxybutyricAcidOverdose.PharmRes.2015Jun;32(6):1894-906.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.1667mL	10.8335mL	21.6671mL
5mM	0.4333mL	2.1667mL	4.3334mL
10mM	0.2167mL	1.0834mL	2.1667mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

KinaseAssay
^[1]

MCTkineticassaysareperformedbymonitoringintracellularpHwithH⁺-sensitivedyeBCECForbydeterminingtheuptakeofl-[¹⁴C]lactate(7.4MBq/mL).Theuptakebuffercontaines75 mMNaCl,2 mMKCl,0.82 mMMgCl₂,1 mMCaCl₂ and20 mMTris/Hepes(pH 7.4).AR-C155858inhibitortitrationsareperformedatpH 6withoocytespreincubatedfor45 mininadifferentuptakebuffer(75 mMNaCl,2 mMKCl,0.82 mMMgCl₂,1 mMCaCl₂ and20 mMMes,pH 6)containingtherequiredconcentrationofAR-C155858priortomeasuringtheuptakeof l-[¹⁴C]lactate(0.5 mM).Unlessstatedotherwise,uptakeisdeterminedover2.5 minforallMCTconstructsexceptforMCT2trnwithorwithoutembiginandMCT2/1withorwithoutembigin,where5and10 minareusedrespectively.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
^[1]

AR-C155858isdissolvedinDMSO.

Theerythrocytes(5%haematocrit)arepre-incubatedfor1 hatroomtemperature(22°C)withorwithoutAR-C155858attherequiredconcentrationbeforeassayingtransportof l-lactate(10mM)at6°C.Initialratesoftransportarecalculatedbyfirst-orderregressionanalysisofthetimecourseofpHchangeandconvertedintonmolofH⁺/minbydeterminingthepHchangeinducedbysmalladditionsofstandardizedNaOH.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].OvensMJ,etal.Theinhibitionofmonocarboxylatetransporter2(MCT2)byAR-C155858ismodulatedbytheassociatedancillaryprotein.BiochemJ.2010Oct15;431(2):217-25.
[2].OvensMJ,etal.AR-C155858isapotentinhibitorofmonocarboxylatetransportersMCT1andMCT2thatbindstoanintracellularsiteinvolvingtransmembranehelices7-10.BiochemJ.2010Jan15;425(3):523-30.
[3].VijayN,etal.ANovelMonocarboxylateTransporterInhibitorasaPotentialTreatmentStrategyforγ-HydroxybutyricAcidOverdose.PharmRes.2015Jun;32(6):1894-906.

MolecularWeight

461.53

Formula

C₂₁H₂₇N₅O₅S

CASNo.

496791-37-8

Storage

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

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

AR-C155858ispreparedasa2.5mg/mLsolutionin10%cyclodextrininnormalsaline^[3].

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

References

[1].OvensMJ,etal.Theinhibitionofmonocarboxylatetransporter2(MCT2)byAR-C155858ismodulatedbytheassociatedancillaryprotein.BiochemJ.2010Oct15;431(2):217-25.
[2].OvensMJ,etal.AR-C155858isapotentinhibitorofmonocarboxylatetransportersMCT1andMCT2thatbindstoanintracellularsiteinvolvingtransmembranehelices7-10.BiochemJ.2010Jan15;425(3):523-30.
[3].VijayN,etal.ANovelMonocarboxylateTransporterInhibitorasaPotentialTreatmentStrategyforγ-HydroxybutyricAcidOverdose.PharmRes.2015Jun;32(6):1894-906.

Purity:95.09%ee.:99.30%

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