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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/AR-C155858/HY-13248/5毫克
商品详细Medchemexpress/AR-C155858/HY-13248/5毫克
Medchemexpress/AR-C155858/HY-13248/5毫克
Medchemexpress/AR-C155858/HY-13248/5毫克
商品编号： HY-13248-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥7560.00
美元价： 4536.00
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
电子邮箱： info@ebiomall.com
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商品介绍
AR-C155858isanovelinhibitorofthemonocarboxylatetransporters(MCTs)MCT1andMCT2(Kivaluesare2.3and< 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(Kivaluesare2.3and<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%inhibitionseenat10nMisfollowedbyagraduallyincreasinginhibitionwhichcanonlybeexplainedbyaKivalueofsignificantlylessthan10nM.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
ConcentrationVolumeMass1mg5mg10mg
1mM2.1667mL10.8335mL21.6671mL
5mM0.4333mL2.1667mL4.3334mL
10mM0.2167mL1.0834mL2.1667mL
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°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
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%