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. 2015 Mar 31;3(2):e00129. doi: 10.1002/prp2.129

Figure 3.

Figure 3

Characterization of LP-925219. (A) Left top, structure of phlorizin. Right bottom, structure of LP-925219, (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-methoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol. (B) Plasma concentrations of LP-925219 measured at various times following an oral dose of 10 mg/kg. C) LP-925219 inhibition of human SGLT1 activity in vitro after washout followed by prolonged recovery time. After cells expressing human SGLT1 were treated with increasing concentrations of LP-925219 for 30 min at 37°C, they were extensively washed, allowed to recover for 18–20 h in cell growth medium, washed again, and then assayed for human SGLT1 activity (Washout). Control cells were incubated in the absence of LP-925219 at 37°C for 30 min, extensively washed, incubated in cell culture medium overnight, washed again, and then assayed for human SGLT1 activity in the presence of increasing concentrations of LP-925219 (No wash). (D) LP-925219 inhibition of human SGLT2 activity in vitro after washout followed by prolonged recovery time. Cells expressing human SGLT2 were studied using the above protocol. (E) Phlorizin inhibition of human SGLT1 activity in vitro after washout followed by prolonged recovery time. Cells expressing human SGLT1 were studied using the above protocol. (F) Phlorizin inhibition of human SGLT2 activity in vitro after washout followed by prolonged recovery time. Cells expressing human SGLT2 were studied using the above protocol.