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Sitagliptin

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
SLC22A8 OAT3 162 CHO-OAT3 Chu, 2007

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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
SLC22A8 OAT3 Sitagliptin 160 Cimetidine CHO-OAT3 Chu, 2007
ABCC2 MRP2, cMOAT Sitagliptin >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Sitagliptin >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC4 MRP4 Sitagliptin >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC22A2 OCT2 Sitagliptin 7.41 Metformin HEK293-OCT2 Hacker, 2015
ABCB11 BSEP Sitagliptin >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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