1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter
  3. VB124

VB124 

Cat. No.: HY-139665
Handling Instructions

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.

For research use only. We do not sell to patients.

VB124 Chemical Structure

VB124 Chemical Structure

CAS No. : 2230186-18-0

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Description

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[1].

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)[1]

In Vitro

VB124 (10 μM) inhibits the cell proliferation of MDA-MB-231 cells, and the cell proliferation rate is less than 50%[1].
VB124 is highly selective for MCT4 over MCT1, showing very little MCT1 inhibitory activity (lactate export IC50=24 μM) in MCT1-expressing BT20 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VB124 (30 mg/kg; p.o.; daily for 28 days) attenuates 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

426.89

Formula

C₂₃H₂₃ClN₂O₄

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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