VB124

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VB124 是一种具有口服活性的、有效的、选择性的 MCT4 抑制剂。VB124 可特异性抑制 MDA-MB-231 细胞中乳酸涌入和流出，IC50 分别为 8.6 nM 和 19 nM。VB124 对 MCT4 的选择性高于 MCT1。VB124可用于心脏肥大、心力衰竭和代谢的研究。

VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s 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.

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 IC50=24 μM) in MCT1-expressing BT20 cells.

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.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.

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Membrane Transporter/Ion Channel

Monocarboxylate Transporter

Monocarboxylate transporter

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2230186-18-0

426.89

C23H23ClN2O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (234.25 mM; 超声助溶 )

CC(C)(OCc1cc(-c2cccc(OC3CC3)c2)n(n1)-c1ccccc1Cl)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years