Description | AR-C155858isanovelinhibitorofthemonocarboxylatetransporters(MCTs)MCT1andMCT2(Kivaluesare2.3and<10=""nm,=""respectively),=""and=""exhibits=""no=""activity=""at=""mct4.=""> |
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IC50&Target | Ki:2.3nM(MCT1),10nM(MCT2) |
InVitro | AR-C155858(10nM-100nM)inhibitsMCT1/MCT2C-terminalchimaeras[1].AR-C155858inhibitsMCT2,andthe70%inhibitionseenat10nMisfollowedbyagraduallyincreasinginhibitionwhichcanonlybeexplainedbyaKivalueofsignificantlylessthan10nM.AR-C155858inhibitsMCT1expressedinXenopusoocytesinatime-andconcentration-dependentmanner[2]. |
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PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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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. | ||||||||||||||||
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MolecularWeight | 461.53 | ||||||||||||
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Formula | C₂₁H₂₇N₅O₅S | ||||||||||||
CASNo. | 496791-37-8 | ||||||||||||
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | 10mMinDMSO AR-C155858ispreparedasa2.5mg/mLsolutionin10%cyclodextrininnormalsaline[3]. *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> | ||||||||||||
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Purity:95.09%ee.:99.30%
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