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7ACC2

CAS No. : 1472624-85-3

MCE 国际站：7ACC2

产品活性：7ACC2 是一种有效的单羧酸盐转运蛋白 (MCT) 抑制剂，IC₅₀ 为 11 nM，可抑制乳酸涌入。7ACC2 还是一种线粒体丙酮酸转运 (mitochondrial pyruvate transport) 的有效抑制剂。7ACC2 通过抑制乳酸通量来发挥抗癌作用。

研究领域：Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease

作用靶点：Monocarboxylate Transporter  |  Mitochondrial Metabolism

In Vitro: 7ACC2 (compound 19; 72 hours) inhibits SiHa cells proliferation in lactate-containing medium with an EC50 of 0.22 μM. In SiHa cells, lactate uptake primarily depends on the high affinity MCT1 transporter.
7ACC2 (compound 19) shows an excellent chemical stability in simulated gastric (SGF) and intestinal (SIF) fluids, a good apparent permeability coefficient (Papp) through Caco-2 monolayer and a high metabolic stability on mouse (MLM) and human liver microsomes (HLM) as well as on human hepatocytes.
7ACC2 is a potent inhibitor of mitochondrial pyruvate transport which consecutively blocks extracellular lactate uptake by promoting intracellular pyruvate accumulation.

In Vivo: 7ACC2 (3 mg/kg; intraperitoneal administration; daily; for 5 days or 10days) treatment significantly inhibits tumor growth in mice. 7ACC2 radiosensitizes tumor cells by reducing hypoxia in vivo.
The intraperitoneal administration of 7ACC2 (compound 19; 3 mg/kg) to mice leads to a C_max of 1246 ng/ml (4 μM) in a very short time (T_max=10 min) associated with a plasma half-life of 4.5 h.

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