| Name | VB124 |
| Description | 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 selective for MCT4 over MCT1 and shows minimal MCT1 inhibitory activity in MCT1-expressing BT20 cells (IC50 value of 24 μM). |
| 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). [1] |
| 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. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 90 mg/mL (210.8 mM), Sonication is recommended.
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| Keywords | VB124 | VB-124 | VB 124 |
| Inhibitors Related | 7ACC1 | BAY-8002 | AZD0095 | MCT1-IN-3 | Niflumic acid | D-Phenylalanine | AZD3965 | MSC-4381 | α-Cyano-4-hydroxycinnamic acid | 7ACC2 | AR-C155858 | Lactate transportor 1 |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
