VB124
目录号: PL07526 纯度: ≥99%
CAS No. :2230186-18-0
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中文名称
VB124
英文名称
VB124
英文别名
2-[[1-(2-Chlorophenyl)-5-[3-(cyclopropyloxy)phenyl]-1H-pyrazol-3-yl]methoxy]-2-methylpropanoic acid;BDBM356744;VB124;US10214492, Example 110
Cas No.
2230186-18-0
分子式
C23H23ClN2O4
分子量
426.89
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
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)
体外研究(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 IC50=24 μM) in MCT1-expressing BT20 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (234.25 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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