VB124

VB124 is a potent and selective MCT4 inhibitor. VB124 might redirect glycolytic carbon flux into mitochondrial pyruvate oxidation. VB124 bolcks lactate import (IC50=8.6nM), and export (IC50=19nM) in MDA-MB-231 cells that are engineers to express MCT4 as the only major plasma membrane lactate transporter.

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monocarboxylate Transporter

Research Areas >> Cardiovascular Disease

VB124 （10 μM） inhibits the cell proliferation of MDA-MB-231 cells, and the cell proliferation rate is less than 50%[1]. Cell Proliferation Assay[1] Cell Line: MDA-MB-231 cells Concentration: 10 μM Incubation Time: Result: Inhibited the cell proliferation of MDA-MB-231 cells (proliferation rate：＜50%).

VB124 (30 mg/ kg; twice per day for 180 days) has no effect on body, heart, liver, or lung weight of mice, suggesting no overt toxicities[1]. VB124 (30 mg/kg; p.o.; daily for 28 days) attenuates isoproterenol-induced cardiac hypertrophy in mice[1]. Animal Model: 12 weeks old C57BL/6 mice[1] Dosage: 30mg/kg Administration: Oral gavage; daily for 28 days (dissolved in 0.5% methylcellulose and 0.1% Tween-20) Result: Prevented cardiac hypertrophy in mice

[1]. [1] Cluntun AA, et.al. The pyruvate-lactate axis modulates cardiac hypertrophy and heart failure. Cell Metab. 2021 Mar 2;33(3):629-648.e10.