VB124

Research use only, not for human use.

VB124 is an orally active, potent and selective MCT4 inhibitor. VB124 blocked lactate import (IC50 value of 8.6 nM) and export (IC50 value of 19 nM) in MDA-MB-231 cells.

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.

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.

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.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.

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Membrane Transporter/Ion Channel

Monocarboxylate Transporter

Monocarboxylate transporter

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2230186-18-0

426.89

C23H23ClN2O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (234.25 mM; Ultrasonic )

CC(C)(OCc1cc(-c2cccc(OC3CC3)c2)n(n1)-c1ccccc1Cl)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years