货号	规格	价格	上海	北京	珠海	重庆	武汉
S89692-5mg买3赠1	99.20%	￥1700.00 S89692-5mg ￥1700.00 现货（买3赠1）	6 6	-	-	-	-
S89692-10mg买3赠1	99.20%	￥2720.00 S89692-10mg ￥2720.00 现货（买3赠1）	5 5	-	-	-	-
S89692-25mg	99.20%	￥5440.00 S89692-25mg ￥5440.00 现货	2 2	-	-	-	-
S89692-100mg	≥98%	￥13800.00 S89692-100mg ￥13800.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

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);Monocarboxylatetransporter

体外研究：

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.

体内研究：

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.

参考文献：

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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.343 ml	11.713 ml	23.425 ml
5 mM	0.469 ml	2.343 ml	4.685 ml
10 mM	0.234 ml	1.171 ml	2.343 ml
50 mM	0.047 ml	0.234 ml	0.469 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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