| Size | Price | Stock | Qty |
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| 10mg |
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| 100mg |
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| Targets |
VB124 targets monocarboxylate transporter 4 (MCT4). MCT4 is a transmembrane protein that mediates the efflux of lactate from cells, playing a critical role in the metabolic adaptation of cancer cells to hypoxia. VB124 functions as a potent and selective MCT4 inhibitor. It is selective for MCT4 over MCT1.
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| ln Vitro |
MDA-MB-231 cells' ability to proliferate is inhibited by VB124 (10 μM), with a cell proliferation rate of less than 50%[1]. VB124 exhibits minimal MCT1 inhibitory activity (lactate output IC50=24 μM) in MCT1-expressing BT20 cells and is more selective for MCT4 than MCT1 [1].
In vitro, VB124 blocks lactate import (IC50 = 8.6 nM) and export (IC50 = 19 nM) in MDA-MB-231 cells. It shows minimal MCT1 inhibitory activity in MCT1-expressing BT20 cells (IC50 = 24 μM). VB124 redirects glycolytic carbon flux into mitochondrial pyruvate oxidation. |
| ln Vivo |
VB124 (30 mg/kg; oral; once daily for 28 days) reduces isoproterenol-induced cardiac hypertrophy in mice [1]. VB124 (30 mg/kg; twice daily for 180 days) had no effect on body, heart, liver, or lung weight in mice, indicating no apparent toxicity [1].
Specific in vivo activity data for VB124 are not extensively reported. As an orally active MCT4 inhibitor, it would be expected to modulate lactate metabolism in vivo. Further studies would be required to evaluate its efficacy in cancer models. |
| Enzyme Assay |
MCT4 transport activity is measured using lactate uptake or efflux assays in MCT4-expressing cells. VB124 is incubated with cells at varying concentrations, and lactate transport is measured using radiolabeled lactate or fluorescence-based methods. IC50 values are calculated from dose-response curves.
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| Cell Assay |
The cellular activity of VB124 is evaluated in MCT4-expressing cancer cell lines such as MDA-MB-231 cells. Cells are treated with the compound, and lactate import and export are measured. Cell viability and metabolic flux are assessed. Lactate levels in the culture medium are measured using enzymatic assays or LC-MS/MS.
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| Animal Protocol |
Animal/Disease Models: 12weeks old C57BL/6 mice[1]
Doses: 30 mg/kg Route of Administration: po (oral gavage); one time/day for 28 days (dissolved in 0.5% methylcellulose and 0.1% Tween-20 ) Experimental Results: Prevention of cardiac hypertrophy in mice. In vivo efficacy of VB124 would typically be evaluated in xenograft mouse models of cancer. Animals would be administered the compound orally, and tumor growth and lactate metabolism would be assessed. Tumor lactate levels and MCT4 expression would be measured as pharmacodynamic endpoints. |
| ADME/Pharmacokinetics |
VB124 has a molecular formula of C23H23ClN2O4 and a molecular weight of 426.89 g/mol. Its SMILES is CC(C)(OCC1=NN(C2=CC=CC=C2Cl)C(C3=CC(OC4CC4)=CC=C3)=C1)C(O)=O. Purity is typically >99%. The compound is soluble in DMSO. It is stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for VB124 are limited. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
VB124 is a potent and selective MCT4 inhibitor. It specifically inhibits lactate efflux and redirects glycolytic carbon flux into mitochondrial pyruvate oxidation. The compound is a valuable tool for studying cancer metabolism and MCT4 function. It has potential applications in research on cardiac hypertrophy and heart failure.
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| Molecular Formula |
C23H23CLN2O4
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|---|---|
| Molecular Weight |
426.8927
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| Exact Mass |
392.17
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| Elemental Analysis |
C, 70.39; H, 6.16; N, 7.14; O, 16.31
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| CAS # |
2230186-18-0
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| Related CAS # |
2230186-18-0; 2230186-91-9 (methyl-VB124);
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| Appearance |
White to off-white solid powder
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| LogP |
4.6
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| InChi Key |
VDUYBQLCMARXKM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24N2O4/c1-23(2,22(26)27)28-15-17-14-21(25(24-17)18-8-4-3-5-9-18)16-7-6-10-20(13-16)29-19-11-12-19/h3-10,13-14,19H,11-12,15H2,1-2H3,(H,26,27)
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| Chemical Name |
2-((5-(3-cyclopropoxyphenyl)-1-phenyl-1H-pyrazol-3-yl)methoxy)-2-methylpropanoic acid
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| Synonyms |
VB124; VB 124; VB-124;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~234.25 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.86 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3425 mL | 11.7126 mL | 23.4252 mL | |
| 5 mM | 0.4685 mL | 2.3425 mL | 4.6850 mL | |
| 10 mM | 0.2343 mL | 1.1713 mL | 2.3425 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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