TABLE 2

In vitro substrates of human OAT2

Compound TypeSubstrateCell SystemVariantKmOAT1 Substrate OAT3 SubstrateReference
µMKm (µM)Km (µM)
Therapeutics
 AntibioticsCefotaximeHEK293 cellsOAT2-546aaUnknownYes (549 and 717)Yee et al., 2013
ErythromycinX. laevis oocytesOAT2-548aa18.5UnknownUnknownKobayashi et al., 2005b
TetracyclineMouse S2 RPTCsUnknown440UnknownYes (556)Babu et al., 2002
 Antigout and uricosuric agentsAllopurinolX. laevis oocytesOAT2-548aaUnknownUnknownKobayashi et al., 2005a
 Antimetabolites5-FluorouracilX. laevis oocytesOAT2-548aa0.0538UnknownUnknownKobayashi et al., 2005a
MethotrexateMouse S2 RPTCsUnknownYes (554 and 724)Yes (10.9–70.6)Sun et al., 2001
 AntiviralsAcyclovirHEK293 cellsOAT2-546aa94Yes (289–839)Yes (416–772)Cheng et al., 2012
GanciclovirHEK293 cellsOAT2-546aa264Yes (896)UnknownCheng et al., 2012
PCVHEK293 cellsOAT2-546aa284UnknownUnknownCheng et al., 2012
 Dietary Supplements and vitaminsAscorbic acid (vitamin C)X. laevis oocytesOAT2-548aaUnknownUnknownKobayashi et al., 2005a
 DiureticsBumetanideX. laevis oocytesOAT2-548aa7.52YesYes (1.6)Kobayashi et al., 2005a
 H2 receptor antagonistsCimetidineHEK293 cellsOAT2-546aaYesUnknownTahara et al., 2005
RanitidineHEK293 cellsOAT2-546aa396YesUnknownTahara et al., 2005
 Herbal medicationsTanshinolHEK293 cellsOAT2-546aa859Yes (121)Yes (1,888)Jia et al., 2015
 MethylxanthinesTheophylline (1,3-DMX)X. laevis oocytesOAT2-548aa12.6UnknownUnknownKobayashi et al., 2005b
XanthineHEK293 cellsOAT2-546aaUnknownUnknownYamada et al., 2014
 Nonsteroidal anti-inflammatory drugsDiclofenacHEK293 cellsOAT2-546aa46.8NoNoZhang et al., 2016
Diclofenac acyl glucuronideHEK293 cellsOAT2-546aa8.6Yes (60.2)Yes (114)Zhang et al., 2016
Salicylic acidMouse S2 RPTCsOAT2-539aaYesYesIgarashi et al., 2002
 Nucleoside reverse transcriptase inhibitorsZidovudineMouse S2 RPTCsUnknown26.8Yes (45.9)Yes (145)Takeda et al., 2002
 TaxanesPaclitaxelX. laevis oocytesOAT2-548aa0.143UnknownUnknownKobayashi et al., 2005a
 Topoisomerase InhibitorsIrinotecanHEK293 cellsOAT2-546aa42.4UnknownUnknownMarada et al., 2015
Endogenous compounds
 AndrogensDHEA sulfateX. laevis oocytesOAT2-548aaUnknownUnknownKobayashi et al., 2005a
 EstrogensE3SX. laevis oocytesOAT2-548aaUnknownUnknownKobayashi et al., 2005a
 None1-Methyl-4-phenylpyridiniumHEK293 cellsOAT2-546aaUnknownUnknownShen et al., 2015
cGMPHEK293 cellsOAT2-546aa101YesYesMarada et al., 2015
cGMPHEK293 cellsOAT2-546aa88Cropp et al., 2008
cGMPHEK293 cellsOAT2-546aaHenjakovic et al., 2015
CreatinineHEK293 cellsOAT2-546aa795UnknownYesShen et al., 2015
CreatinineHEK293 cellsOAT2-546aa986Lepist et al., 2014
Orotic acidHEK293 cellsOAT2-546aa200 (rOat2)UnknownUnknownFork et al., 2011
PAHOther cellsUnknownYes (3.1–60.3)Yes (7.4 and 87.2)Sun et al., 2001
Uric acidHEK293 cellsOAT2-546aaUnknownUnknownHenjakovic et al., 2015
 ProstaglandinsProstaglandin E2X. laevis oocytesOAT2-548aaUnknownUnknownKobayashi et al., 2005a
Prostaglandin F2Mouse S2 RPTCsOAT2-539aa0.425UnknownUnknownEnomoto et al., 2002b
Prostaglandin F2HEK293 cellsOAT2-546aa45.5UnknownUnknownJia et al., 2015
Prostaglandin F2Other cellsunknownUnknownUnknownNakagomi-Hagihara et al., 2007