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VB124

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Catalog No. T60165Cas No. 2230186-18-0

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).

VB124

VB124

😃Good
Purity: 99.57%
Catalog No. T60165Cas No. 2230186-18-0
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).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$122In StockIn Stock
5 mg$297In StockIn Stock
10 mg$428In StockIn Stock
25 mg$826In StockIn Stock
50 mg$1,290In StockIn Stock
100 mg$1,760-In Stock
1 mL x 10 mM (in DMSO)$336In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.57%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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).
Targets&IC50
MCT1:24 mM, MDA-MB-231 cells:8.6 nM
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]
Chemical Properties
Molecular Weight426.89
FormulaC23H23ClN2O4
Cas No.2230186-18-0
SmilesCC(C)(OCc1cc(-c2cccc(OC3CC3)c2)n(n1)-c1ccccc1Cl)C(O)=O
Relative Density.1.31 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 125 mg/mL (292.82 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3425 mL11.7126 mL23.4252 mL117.1262 mL
5 mM0.4685 mL2.3425 mL4.6850 mL23.4252 mL
10 mM0.2343 mL1.1713 mL2.3425 mL11.7126 mL
20 mM0.1171 mL0.5856 mL1.1713 mL5.8563 mL
50 mM0.0469 mL0.2343 mL0.4685 mL2.3425 mL
100 mM0.0234 mL0.1171 mL0.2343 mL1.1713 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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