Transporter |
% Control Activitya |
Probe Substrate |
Remogliflozin Etabonate |
Remogliflozin |
GSK279782 |
GSK333081 |
OAT 1 |
102 (5.2) |
101 (4.1) |
105 (2.5) |
107 (5.4) |
[14C]-p-aminohippuric acid |
OAT 2 |
122 (3.4) |
84.3 (3.5) |
87.2 (1.4) |
82.5 (1.5) |
[3H]-prostaglandin F2α |
OAT 3 |
84.4 (1.9) |
110 (0.6) |
112 (3.7) |
115 (1.9) |
[3H]-estrone sulfate |
OAT 4 |
96.3 (1.5) |
99.6 (2.1) |
89.5 (0.5) |
93.0 (2.0) |
[3H]-estrone sulfate |
OCT 1 |
44.6 (4.6) |
84.0 (3.2) |
74.0 (3.1) |
72.2 (9.8) |
[14C]-tetraethylammonium |
OCT 2 |
105 (2.1) |
107 (3.5) |
98.3 (7.2) |
113 (0.7) |
[14C]-tetraethylammonium |
OCT 2A |
98.9 (1.6) |
112 (3.2) |
112 (1.5) |
102 (2.7) |
[14C]-tetraethylammonium |
OCT 3 |
73.8 (3.6) |
62.9 (1.7) |
87.5 (2.9) |
69.0 (0.7) |
[3H]-histamine |
URAT1 |
106 (2.6) |
112 (2.5) |
111 (4.4) |
112 (2.5) |
[14C]-uric acid |
aData are the mean (± standard deviation) from triplicate well from a single concentration screening experiment. Inhibition of more than 20% was considered notable and
observed for OCT 1 and 3. Therefore, a subsequent study was completed to determine an IC50 values reported in Table 1. |
