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.
Table 2: Inhibition of Human Solute Carriers by 30 μM Remogliflozin etabonate, Remogliflozin and Metabolites.