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Zafirlukast

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 Zafirlukast 9.7 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 Wittwer, 2013
SLC47A1 MATE1 Zafirlukast 1.3 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
SLC47A2 MATE2K Zafirlukast 7.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE2K Wittwer, 2013
SLCO2B1 OATP2B1, OATP-B Zafirlukast 1.4 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
ABCC2 MRP2, cMOAT Zafirlukast 58.8 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Zafirlukast 12.1 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Zafirlukast >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLCO1B3 OATP1B3, OATP8 Zafirlukast 4.96 FMTX CHO-OATP1B3 Leibovici, 1989
ABCB11 BSEP Zafirlukast 11.1 Taurocholate Sf9 cell membrane vesicles Morgan, 2013

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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