VB124

SKU: orb1689793

Description

VB124 is a potent and selective oral MCT4 inhibitor that blocks lactate transport in cancer cells. It is used in oncology research to investigate metabolic targeting in tumors, with supporting in vitro data from models like MDA-MB-231 and BT20 cells.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2230186-18-0
• MW: 426.89
• Purity: 99.57% (May vary between batches)
• Formula: C₂₃H₂₃ClN₂O₄
• SMILES: CC(C)(OCc1cc(-c2cccc(OC3CC3)c2)n(n1)-c1ccccc1Cl)C(O)=O
• Target: Monocarboxylate transporter
• Solubility: DMSO:125 mg/mL (292.82 mM)

Bioactivity

• Target IC50:
  MCT1:24 mM|MDA-MB-231 cells:8.6 nM
• In Vivo:
  METHODS: Mice were treated with a supramaximal dose of VB124 (30 mg/kg twice daily for 180 days) and the effects on body, heart, liver, or lung weights were observed. RESULTS VB124 had no effect on body, heart, liver, or lung weights. METHODS: Osmotic minipumps were surgically implanted to continuously deliver ISO to induce hypertrophy in mice, and these mice were simultaneously treated with VB124 (30 mg/kg) by daily oral gavage for 4 weeks. We performed echocardiography on these mice at the end of 4 weeks and collected their hearts after sacrifice. RESULTS VB124 treatment ameliorated mitochondrial structural aberrations, and MCT4 inhibition reversed many of the pathological features of ISO-induced cardiac hypertrophy, including metabolic perturbations and mitochondrial structural damage.
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• In Vitro:
  VB124 blocks lactate import (IC50 of 8.6 nM) and export (IC50 of 19 nM) in MDA-MB-231 cells engineered to express MCT4 as the sole major plasma membrane lactate transporter; VB124 is selective for MCT4 over MCT1 and shows minimal MCT1 inhibitory activity in MCT1-expressing BT20 cells (IC50 of 24 μM).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

VB 124, VB124, VB-124, MCT4, Monocarboxylatetransporter, Monocarboxylate transporter

Compound Identifiers

PubChem CID

134602985