VB124
规格
| Cas Number | 2230186-18-0(DMSO) |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 过滤标签 | Monocarboxylate Transporter,膜转运器/离子通道,Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | VB124 是一种口服活性、强效和选择性 MCT4 抑制剂。VB124 能特异性地抑制乳酸外流，在 MDA-MB-231 细胞中乳酸输入和输出的 IC 50 s 分别为 8.6 nM 和 19 nM。VB124 对 MCT4 的选择性高于 MCT1。 |
| 英文描述 |
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. 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) |