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Lesinurad is an inhibitor of urate anion transporter 1 (URAT1; IC50s = 3.5 and 81 µM for human and rat transporters, respectively), a transporter that prevents renal urate resorption.1 It decreases uptake of urate by MDCK cells transfected with human URAT1.2 Lesinurad (80 mg/kg) also decreases serum levels of uric acid and urea nitrogen in a rat model of gout. Formulations containing lesinurad have been used in combination with other compounds in the treatment of gout.
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1. Mechanism of high affinity inhibition of the human urate transporter URAT1. Sci. Rep. 6:34995, (2016).
2. Identification and characterization of a potent and selective inhibitor of human urate transporter 1. Pharmacol. Rep. (2017).