生物活性 | |||
---|---|---|---|
描述 | The nuclear receptors REV-ERBα and -β link circadian rhythms and metabolism. SR-9009 is a potent synthetic REV-ERB agonist with IC50 value of 710nM for suppression of transcription in a cotransfection assay using full-length REV-ERB-a along with a luciferase reporter driven by the Bmal1 promoter. Administration of SR-9009 at dose of 100mg/kg, i.p., b.i.d., for 30 days resulted in a decrease in fat mass and in plasma lipids in diet-induced obese mice. SR9009 at concentration ranging in 2.5-20μM dose-dependently decreased mESC viability, rewired cellular metabolism shown by reduction of mitochondrial respiration, both of which were independent of REV-ERBs, and altered gene transcription in hepatocytes and embryonic stem cells lacking both REV-ERBα and –β, suggesting SR9009 may not be used solely as surrogate for REV-ERB activity. | ||
作用机制 | SR-9009 directly binds to REV-ERB-α.[1] |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.28mL 0.46mL 0.23mL |
11.42mL 2.28mL 1.14mL |
22.83mL 4.57mL 2.28mL |
参考文献 |
---|