VB124 (C09-1184-953)

VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC 50 s 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 metabolismIn VitroVB124 (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 IC 50 =24 μM) in MCT1-expressing BT20 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoVB124 (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 12 weeks old C57BL/6 mice Dosage: 30 mg/kg Administration: Oral gavage; daily for 28 days (dissolved in 0.5% methylcellulose and 0.1% Tween-20) Result: Prevented cardiac hypertrophy in mice.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). Specification: 10mM in DMSO Molecular Formula: C23H23ClN2O4 Molecular Weight: 426.89