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| 货号 | 产品名 | 中文名称 | 产品描述 |
|---|---|---|---|
| SJ-MX3529 | SR9011 | SR9011 is a novel and potent synthetic REV-ERBα/β agonist with IC50 values of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. Synchronizing rhythms of behaviour and metabolic processes is important for cardiovascular health and preventing metabolic diseases. The nuclear receptors REV-ERB-α and REV-ERB-β have an integral role in regulating the expression of core clock proteins driving rhythms in activity and metabolism. Administration of synthetic REV-ERB ligands alters circadian behaviour and the circadian pattern of core clock gene expression in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also altered, resulting in increased energy expenditure. Treatment of diet-induced obese mice with a REV-ERB agonist decreased obesity by reducing fat mass and markedly improving dyslipidaemia and hyperglycaemia. These results indicate that synthetic REV-ERB ligands that pharmacologically target the circadian rhythm may be beneficial in the treatment of sleep disorders as well as metabolic diseases. | |
| SJ-MX3931 | SR8278 | SR8278 是一种竞争性核血红素受体 REV-ERB 合成拮抗剂。SR8278 抑制 REV-ERBα 转录活性，EC50 为 0.47 μM。SR8278 用于调节生物体内的代谢和研究生物节律。 |
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