An OAT inhibitor
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Steviol is the aglycon derivative of steviol glycosides, which are natural sweeteners isolated from S. rebaudiana. Steviol inhibits human organic anion transporters (hOATs) in uptake assays using murine cells from the S2 segment of proximal tubules. It is selective for hOAT1 and hOAT3 over hOAT2 and hOAT4 (IC50s = 11.4, 36.5, 1,000, and 285 μM, respectively). Uptake assays in mouse renal cortical slices yield similar results with IC50 values of 12.8 and 67.6 μM for hOAT1 and hOAT3, respectively. Due to the use of steviol glycosides as sweeteners, the safety of steviol is widely studied, including its genotoxicity and toxicokinetics.
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