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Tacrine

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
SLC47A1 MATE1 Tacrine 0.51 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE1 Astorga, 2012
SLC47A2 MATE2K Tacrine 1.1 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE2K Astorga, 2012
SLC22A2 OCT2 Tacrine 2.3 1-methyl-4-phenylpyridinium (MPP+) CHO-OCT2 Sandoval, 2018
SLC22A1 OCT1 Tacrine 83 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Kido, 2011
SLC47A1 MATE1 Tacrine 1.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Kido, 2011
SLC47A2 MATE2K Tacrine 100 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Kido, 2011
SLC22A1 OCT1 Tacrine 21.72 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
SLC22A2 OCT2 Tacrine 0.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) CHO-OCT2 Sandoval, 2018
ABCC4 MRP4 Tacrine 23.7 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC2 MRP2, cMOAT Tacrine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Tacrine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Tacrine 0.6 Metformin CHO-OCT2 Sandoval, 2018
SLC22A2 OCT2 Tacrine 1 NBD-MTMA CHO-OCT2 Sandoval, 2018
ABCB11 BSEP Tacrine >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Tacrine 0.9 Tetraethylammonium CHO-OCT2 Sandoval, 2018

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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