urat-1 inhibitor 1

URAT1 inhibitor 1 (1g) is a potent inhibitor of uric acid transporter 1 (URAT1) with an IC50 of 32 nM, and has potential therapeutic applications for treating hyperuricemia associated with gout.

Compound 27b, also known as hURAT1 inhibitor 1, is an isomarine-derived, orally active inhibitor that targets both hURAT1 and GLUT9 with IC50 values of 0.16 μM and 4.47 μM, respectively. This compound exhibits significant anti-hyperuricemia effects and has demonstrated potent uric acid-lowering activity in a hyperuricemia mouse model at a dose of 10 mg/kg. Importantly, Compound 27b displays no notable in vitro cytotoxicity or in vivo hepatotoxicity, and possesses favorable pharmacokinetic (PK) characteristics.

URAT1 inhibitor11 (Compound 7) is a potent URAT1 inhibitor, exhibiting an IC50 of 0.18 μM. It effectively reduces uric acid levels in zebrafish with hyperuricemia induced by Potassium oxonate and Xanthinesodium salt.

URAT1 inhibitor13 (compound 22k) is a potent inhibitor of URAT1, useful for research related to gout.

URAT1 inhibitor10 (Compound 23a) is a URAT1 inhibitor with an IC50 of 0.052 μM. It exhibits oral efficacy and low cytotoxicity. The compound demonstrates high selectivity for OAT1, with an IC50 of 9.17 μM.