VB124 is an orally active, potent, and selective MCT4 inhibitor, demonstrating specificity in hindering lactate efflux, with IC50 values of 8.6 nM and 19 nM for lactate import and export, respectively, in MDA-MB-231 cells. Its high selectivity for MCT4 over MCT1 positions VB124 as a promising agent for researching cardiac hypertrophy, heart failure, and metabolic disorders [1].

VB124 (10 μM) inhibits the cell proliferation of MDA-MB-231 cells, and the cell proliferation rate is less than 50% [1]. VB124 is more selective to MCT4 than MCT1, exhibiting very little MCT1 inhibitory activity (lactate export IC 50 =24 μM) in MCT1-expressing BT20 cells [1].

VB124, administered orally at a dosage of 30 mg/kg daily for 28 days, effectively mitigates isoproterenol-induced cardiac hypertrophy in 12-week-old C57BL/6 mice, as evidenced by a study [1]. The same compound at the same dosage, when given twice daily for 180 days, demonstrated no significant impact on the body, heart, liver, or lung weight in mice, indicating a lack of overt toxicities [1]. The administration involved oral gavage of VB124 dissolved in 0.5% methylcellulose and 0.1% Tween-20, underscoring its efficacy in preventing cardiac enlargement without apparent toxicity.