URAT1 inhibitor 3

URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi.

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 IC₅₀ values of 10.16 μM and 4.04 μM of OAT1 and ABCG2, respectively^[1].

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].

References:
[1]. Zhao Z, et, al. Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents. Eur J Med Chem. 2022 Nov 15;242:114682.