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Mexiletine

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.


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In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
SLC22A2 OCT2 Mexiletine 50.4 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Sandoval, 2018
SLC22A2 OCT2 Mexiletine 19.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) CHO-OCT2 Sandoval, 2018
ABCC2 MRP2, cMOAT Mexiletine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Mexiletine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Mexiletine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Mexiletine 21.5 Metformin CHO-OCT2 Sandoval, 2018
SLC22A2 OCT2 Mexiletine 55 N-methylpyridinium HEK293-OCT2 Zolk, 2009
SLC22A2 OCT2 Mexiletine 30.5 NBD-MTMA CHO-OCT2 Sandoval, 2018
ABCB11 BSEP Mexiletine >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Mexiletine 28.5 Tetraethylammonium CHO-OCT2 Sandoval, 2018

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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