URAT1 inhibitor 3 is a potent, orally active, selective inhibitor of URAT1(IC 50 = 0.8 nM). URAT1 inhibitor 3 shows urate-lowering efficacy that can be used in gout and hyperuricemi research [1].

URAT1 inhibitor 3 (0-400 μM; 24 and 72 h; HepG2 and HK2 cells) has low toxicity and inhibits cell viability at high concentrations [1]. URAT1 inhibitor 3 (0.01-100 μM) has lower inhibition on urate excretion transporters with IC 50 values of 10.16 μM and 4.04 μM of OAT1 and ABCG2, respectively [1]. Cell Viability Assay [1] Cell Line: HepG2 and HK2 cells Concentration: 0, 100, 200, 300, and 400 μM Incubation Time: 24 and 72 hours Result: Had little cytotoxicity at 24 h and inhibition rate of 34.75% and 35.9% of HepG2 and HK2 cells, respectively.

URAT1 inhibitor 3 (1-4 mg/kg; i.g.; once) has urate lowering efficacy in a mouse model of hyperuricemia [1]. URAT1 inhibitor 3 (50 mg/kg; i.g.; daily, for 14 d) has no hepatic and renal toxicities in mice [1]. URAT1 inhibitor 3 (50 mg/kg; i.g.; once) induces GSH depletion in Kunming mice with hyperuricemia model [1]. Animal Model: Male Kunming (KM) mice with hyperuricemia model [1] Dosage: 1, 2, and 4 mg/kg Administration: Oral gavage; once Result: Decreased the serum urate levels in a dose-dependent manner. Animal Model: Male Kunming mice [1] Dosage: 50 mg/kg Administration: Oral gavage; daily, for 14 days Result: Did not cause renal toxicity. Animal Model: Male Kunming mice with hyperuricemia model [1] Dosage: 50 mg/kg Administration: Oral gavage; once Result: Decreased the serum GSH levels from 42.23 μM to 20.39 μM.