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Pentamidine

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Km (μM) Cell System Reference
SLC22A1 OCT1 36.4 CHO-OCT1 Ming, 2009

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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
SLC22A1 OCT1 Pentamidine 0.4 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT1 Jung, 2008
SLC22A1 OCT1 Pentamidine 22.1 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Wittwer, 2013
SLC22A3 OCT3 Pentamidine 9.5 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT3 Wittwer, 2013
SLC22A2 OCT2 Pentamidine 1.2 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 Wittwer, 2013
SLC47A1 MATE1 Pentamidine 2.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
SLC47A2 MATE2K Pentamidine 2.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013
SLC47A2 MATE2K Pentamidine 10.4 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013
ABCC2 MRP2, cMOAT Pentamidine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Pentamidine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Pentamidine >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC47A1 MATE1 Pentamidine 0.41 Metformin MDCK2- MATE1 Wittwer, 2013
SLC47A1 MATE1 Pentamidine 2 Metformin HEK293-MATE1 Wittwer, 2013
SLC22A1 OCT1 Pentamidine 16.4 N-methylpyridinium CHO-OCT1 Ming, 2009
SLC22A2 OCT2 Pentamidine 10.6 N-methylpyridinium CHO-OCT2 Ming, 2009
SLC22A3 OCT3 Pentamidine 14.8 N-methylpyridinium CHO-OCT3 Ming, 2009
ABCB11 BSEP Pentamidine >133 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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