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Lesinurad is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout in combination with xanthine oxidase inhibitors. Lesinurad is determined to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with Km values of 0.85 and 2 µM, respectively. Lesinurad (RDEA594) is a potential uric acid lowering agent througn inhibition of uric acid reuptake, and exhibits favorable p450 profiles, inhibits CYP2C9 and CYP2C8 with IC50 of 14.4 μM and 16.2 μM, respectively. IC50s of Lesinurad are all above 100 µM for CYP1A2, CYP2C19, and CYP2D6.
In vivo, Lesinurad (RDEA594) shows better pharmacokinetics than its pro-drug RDEA806. The 100 mg dose of Lesinurad exhibits a phamacological effect in the range of that produced by 300 mg to 800 mg single doses of RDEA806.
| Molecular Weight | 404.28 |
| Formula | C17H14BrN3O2S |
| CAS Number | 878672-00-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage | -20°C |
| Related URAT1 Products |
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| Verinurad
Verinurad, also known as RDEA3170, is an organic anion transporter URAT1 inhibitor with an IC50 of 25 nM. |
| Dotinurad
Dotinurad is a potent selective urate reabsorption inhibitor. Dotinurad inhibits Urate Transporter 1 (URAT1), IC50 value is 37.2 nM. Dotinurad is used as a uric acid-enhancing excretor. |
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