glut9

Fraxin (Fraxoside) is a glucoside of fraxetin.

URAT1/GLUT9-IN-1 (compound 29) effectively inhibits urate transporter 1 (URAT1) with an IC50 value of 2.01 μM and glucose transporter 9 (GLUT9) with an IC50 of 18.21 μM. This compound exhibits favorable pharmacokinetic properties and oral bioavailability, making it useful for research in gout and hyperuricemia.

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.

TRPV1 antagonist 10 is a potent, orally active TRPV1 antagonist with an IC50 of 33.06 nM and serves as a moderate to weak inhibitor of URAT1 (IC50 = 22.51 μM) and GLUT9 (inhibition of 60.25% at 50 μM). It exhibits analgesic and urate-lowering properties and is applicable for research in hyperuricemia and inflammatory pain.

KPH2f, a dual URAT1/GLUT9 inhibitor, demonstrates safety, oral activity, and efficacy, with inhibitory concentrations (IC50s) of 0.24 μM for URAT1 and 9.37 μM for GLUT9. It exhibits minimal effects on OAT1 and ABCG2, with IC50 values of 32.14 μM and 26.74 μM, respectively [1].