| S4640 |
Lesinurad |
Lesinurad (RDEA-594) is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout in combination with xanthine oxidase inhibitors. Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 μM, respectively. |
Selective |
|
| S8736 |
Verinurad (RDEA3170) |
Verinurad (RDEA3170) is a high-affinity inhibitor of the URAT1 transporter with an IC50 of 25?nM for inhibiting transport activity of human URAT1. It inhibits the related URAT1 homologs OAT4 and OAT1 with approximately 200-fold lower affinity compared to URAT1 with IC50 values of 5.9?μM and 4.6?μM, respectively. |
Selective |
URAT1 transporter, IC50: 25 nM |
| S5189 |
Lesinurad sodium |
Lesinurad (Selexipag, RDEA-594) sodium (Zurampic) is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout. Lesinurad sodium inhibits the uric acid transporter URAT1 and Kidney transporter OAT with IC50/Km of 4.3 μM/0.85 μM and 3.5 μM/2 μM for OAT1 and OAT3, respectively. |
Pan |
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