2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Lesinurad sodium (RDEA594 sodium) is an once-daily inhibitor of URAT1; URAT1 is a transporter in the kidney that regulates uric acid excretion from the body.
IC50 Value:
in vivo: In healthy subjects, the combination of 40 mg FBX with RDEA-594 reduced sUA by approximately 70% at the 200 mg and 400 mg RDEA-594 dose levels, respectively. In gout patients, FBX 40 mg and 80 mg alone reduced sUA by 35% and 47%, respectively. FBX 40 mg + RDEA-594 reduced sUA by 56% and 61% when combined with RDEA-594 400 mg or 600 mg. respectively, resulting in response rates of 100% for sUA <6 and <5 mg/dl and 64% <4 mg/dl. FBX 80 mg + RDEA-594 reduced sUA by 65% and 73% when combined with RDEA-594 400 mg or 600 mg respectively. Following single dosing of RDEA594, exposure of RDEA594 was significantly higher than those obtained from RDEA 806 dosing, >5X at 20 mg/kg in rats and >10X at 30 mg/kg in monkeys.
Clinical trial: Lesinurad and Febuxostat Combination Extension Study in Gout .Phase3
