VB124 是一种具有口服活性的、有效且选择性的MCT4抑制剂。VB124 可特异性抑制 MDA-MB-231 细胞中乳酸的涌入和流出，IC50分别为 8.6 nM 和 19 nM。VB124 对 MCT4 的选择性高于 MCT1。VB124可用于心脏肥大、心力衰竭和代谢的研究。

VB124 is an orally active, potent, and selective inhibitor of MCT4. 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 metabolism [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 (30 mg/kg; p.o.; daily for 28 days) reduces isoproterenol-induced cardiac hypertrophy in mice [1]. 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 [1]. Animal Model: 12 weeks old C57BL/6 mice [1] 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.

2230186-18-0

C23H23ClN2O4

426.89

DMSO:90mg/mL (210.8mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years