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SR9011 is a REV-ERB agonist that increases the constitutive repression of genes regulated by REV-ERBα and REV-ERBβ with IC50 values of 790 and 560 nM, respectively.1 It has no activity at other nuclear receptors. SR9011 blocks the activity of the suprachiasmatic nucleus (SCN) clock, with reversible inhibition of circadian oscillation in SCN explants cultured from Per2-luc reporter mice.1 The circadian pattern of expression of several metabolic genes in liver, skeletal muscle, and adipose tissue was also shown to be altered in mice exposed to SR9011, resulting in increased energy expenditure.1
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1. Regulation of circadian behaviour and metabolism by synthetic REV-