VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism.IC50 & Target: IC50: 8.6 nM (lactate import in MDA-MB-231 cells expressing MCT4); 19 nM (lactate export in MDA-MB-231 cells expressing MCT4); 24 μM (lactate export in BT20 cells expressing MCT1)In Vitro: VB124 (10 μM) inhibits the cell proliferation of MDA-MB-231 cells, and the cell proliferation rate is less than 50%.
VB124 is highly selective for MCT4 over MCT1, showing very little MCT1 inhibitory activity (lactate export IC50=24 μM) in MCT1-expressing BT20 cells.In Vivo: VB124 (30 mg/kg; p.o.; daily for 28 days) attenuates isoproterenol-induced cardiac hypertrophy in mice.
VB124 (30 mg/kg; twice per day for 180 days) has no effect on the body, heart, liver, or lung weight of mice, suggesting no overt toxicities.