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Losartan

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
ABCB1 MDR1, P-gp 100 MDR1-containing proteoliposomes Borgnia, 1996
ABCB1 MDR1, P-gp 232 MDR1-expressing Caco-2 cells Soldner, 2000
ABCB1 MDR1, P-gp 403.2 MDR1-expressing MDCK cells Soldner, 2000

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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 Losartan 250 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-MATE1 Wittwer, 2013
SLC22A8 OAT3 Losartan 0.36 6-carboxyfluorescein HEK293-OAT3 Zou, 2021
SLC22A6 OAT1 Losartan 11.4 6-carboxyfluorescein HEK293-OAT1 Zou, 2021
ABCG2 BCRP, MXR Losartan 4.8 Cholecystokinin octapeptide BCRP membrane vesicles Yee, 2021
SLCO2B1 OATP2B1, OATP-B Losartan 8 Dibromofluorescein HEK293-OATP2B1 Unger, 2020
ABCC4 MRP4 Losartan 34.1 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
ABCC3 MRP3 Losartan >133 Estradiol-17beta-glucuronide Sf9 cell membrane vesicles Morgan, 2013
SLC15A1 PEPT1 Losartan 24 Glycylsarcosine Caco-2 Knutter, 2009
SLC15A1 PEPT1 Losartan 52 Glycylsarcosine HeLa-PEPT1 Knutter, 2009
SLC15A2 PEPT2 Losartan 2.4 Glycylsarcosine HeLa-PEPT2 Knutter, 2009
ABCB11 BSEP Losartan 8.53 Taurocholate Sf9 cell membrane vesicles Morgan, 2013
SLC22A12 URAT1 Losartan 0.0077 Uric acid URAT1-expressing oocytes Iwanaga, 2007
ABCC4 MRP4 Losartan 1.5 Uric acid MRP4-expressing Sf9 vesicles Sato, 2008
SLC22A11 OAT4 Losartan 18 Uric acid HEK293-OAT4 Sato, 2008
SLC22A6 OAT1 Losartan 12 Uric acid HEK293-OAT1 Sato, 2008
SLC22A8 OAT3 Losartan 1.6 Uric acid HEK293-OAT3 Sato, 2008
SLC22A12 URAT1 Losartan 570.5 Uric acid HEK293-URAT1 Uetake, 2010

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Clinical Drug-Drug Interactions

No drug-drug interaction information.


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