[CAS NO. 2230186-18-0] VB124
PRODUCTS SPECIFICATIONS [2230186-18-0]
DESCRIPTION [2230186-18-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 426.89 |
| Molecular Formula | C23H23ClN2O4 |
| SMILES | CC(C)(OCC1=NN(C2=CC=CC=C2Cl)C(C3=CC=CC(OC4CC4)=C3)=C1)C(O)=O |
Summary
VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC 50 s 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
IC
50
=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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 234.25 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |