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| Cas No.: | 2230186-18-0 |
| Chemical Name: | VB124 |
| Synonyms: | VB124; VB 124; VB-124 |
| SMILES: | OC(C(C)(C)OCC(C=C1C2=CC(OC3CC3)=CC=C2)=NN1C4=CC=CC=C4)=O |
| Formula: | C23H23ClN2O4 |
| M.Wt: | 426.89 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Publication: | [1]. [1] Cluntun AA, et.al. The pyruvate-lactate axis modulates cardiac hypertrophy and heart failure. Cell Metab. 2021 Mar 2;33(3):629-648.e10. |
| Description: | VB124 is a potent and selective MCT4 inhibitor. VB124 might redirect glycolytic carbon flux into mitochondrial pyruvate oxidation. VB124 bolcks lactate import (IC50=8.6nM), and export (IC50=19nM) in MDA-MB-231 cells that are engineers to express MCT4 as the only major plasma membrane lactate transporter. |
| In Vivo: | VB124 (30 mg/ kg; twice per day for 180 days) has no effect on body, heart, liver, or lung weight of mice, suggesting no overt toxicities[1]. VB124 (30 mg/kg; p.o.; daily for 28 days) attenuates isoproterenol-induced cardiac hypertrophy in mice[1]. Animal Model: 12 weeks old C57BL/6 mice[1] Dosage: 30mg/kg Administration: Oral gavage; daily for 28 days (dissolved in 0.5% methylcellulose and 0.1% Tween-20) Result: Prevented cardiac hypertrophy in mice |
| In Vitro: | VB124 （10 μM） inhibits the cell proliferation of MDA-MB-231 cells, and the cell proliferation rate is less than 50%[1]. Cell Proliferation Assay[1] Cell Line: MDA-MB-231 cells Concentration: 10 μM Incubation Time: Result: Inhibited the cell proliferation of MDA-MB-231 cells (proliferation rate：＜50%). |
| References: | [1]. [1] Cluntun AA, et.al. The pyruvate-lactate axis modulates cardiac hypertrophy and heart failure. Cell Metab. 2021 Mar 2;33(3):629-648.e10. |
MSDS
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| MSDS_31412_DC47562_2230186-18-0 |
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