KPH2f is a novel, orally bioactive and potent dual URAT1/GLUT9 inhibitor with the potential to be used an anti-hyperuricemic agent for gout treatment. It is a verinurad analogthat exhibited URAT1 inhibitory activity with IC50 of 0.24 μM, comparable to that of verinurad (IC50 = 0.17 μM). KPH2f also inhibited GLUT9 with an IC50 value of 9.37 μM, indicating the dual URAT1/GLUT9 targeting capability. KPH2f demonstrated an oral bioavailability of 30.13%, better than that of verinurad (21.47%). KPH2f showed little effects on OAT1 and ABCG2, and thus was unlikely to cause OAT1/ABCG2-mediated drug-drug interactions and/or to neutralize the uricosuric effects of URAT1/GLUT9 inhibitors.
纯度:≥98%