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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related URAT1 Products |
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| KPH2f
KPH2f is an orally potent dual URAT1/GLUT9 inhibitor, with IC50s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively.KPH2f had little effect on OAT1 and ABCG2 (IC50s of 32.14 and 26.74 μM, respectively). |
| URAT1 inhibitor 8
URAT1 inhibitor 8 is a potent URAT1 inhibitor with an IC50 of 0.001 μM.URAT1 inhibitor 8 can be used in gout related studies. |
| URAT1 inhibitor 1
URAT1 inhibitor 1 is a uric acid transporter 1 (URAT1) inhibitor with an IC50 value of 32 nM for inhibition of uric acid transporter 1 (URAT1).It can be used in studies related to hyperuricemia and gout. |
| URAT1 inhibitor 3
URAT1 inhibitor 3 is an orally potent and selective URAT1 inhibitor with an IC50 value of 0.8 nM.URAT1 inhibitor 3 has a uric acid lowering effect and can be used in studies related to gout and hyperuricemia. |
| AR882
AR882 is a potential best-in-class (BIC), selective inhibitor of uric acid transporter protein 1 (URAT1) for studies related to hyperuricemia and gout. |
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