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
In Vitro
VB124 (10 μM) inhibits the cell proliferation of MDA-MB-231 cells, and the cell proliferation rate is less than 50%. 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. 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 12 weeks old C57BL/6 mice 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.
Form:Solid
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)
사양
사양 및 순도
≥98%
생화학 및 생리적 메커니즘
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 .
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What is the purity of this product?
This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.
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Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.
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This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 2230186-18-0, the molecular formula is C23H23ClN2O4, and the molecular weight is 426.89 g/mol.
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