Transporter | Substrate | Percent Inhibition | ||||
---|---|---|---|---|---|---|
Linagliptin | Prototypical Inhibitor | |||||
Mean | SD | Mean | SD | Inhibitor Used | ||
OAT1 | [3H]PAH (0.2 μM) | 1.07 | 8.33 | 96.2 | 0.57 | Probenecid (300 μM) |
OAT3 | [3H]E-sul (0.1 μM) | 0 (–5.70) | 8.71 | 88.5 | 3.45 | Probenecid (100 μM) |
OAT4 | [3H]E-sul (0.1 μM) | 0 (–26) | 7.98 | 81.4 | 2.97 | Probenecid (500 μM) |
OATP1B1 | [3H]E217βG (0.1 μM) | 35.5 | 3.93 | 98.4 | 0.81 | Rifampicin (100 μM) |
OATP1B3 | [3H]CCK8 (0.1 μM) | 3.39 | 5.78 | 97.4 | 2.01 | Rifampicin (100 μM) |
OCTN1 | [3H]Ergothioneine (1 μM) | 19.4 | 3.60 | 83.9 | 0.35 | Quinidine (1500 μM) |
OCTN2 | [3H]Carnitine (0.1 μM) | 15.5 | 1.25 | 89.9 | 0.93 | Quinidine (1500 μM) |
CCK8, cholecystokinin-8; E217βG, estradiol 17β-d-glucuronide; E-sul, estrone 3-sulfate; OAT, organic anion transporter; OATP, organic anion–transporting polypeptide; OCTN, organic cation/carnitine transporter; PAH, aminohippuric acid, SD: standard deviation.