SR 9011 – 6.5mg/.2mL (325mg/10mL)

REV-ERB nuclear receptors have a critical role in feedback regulation of the circadian oscillator. Both Bmal1 and Clock are direct REV-ERB target genes and loss of REV-ERB-α alters circadian behavior.

In vitro: SR9011 dose-dependently increased the REV-ERB-dependent repressor activity assessed in HEK293 cells. In addition, SR9011 potently and efficaciously suppressed transcription in a transfection assay using full-length REV-ERB-a along with a luciferase reporter driven by the Bmal1 promoter.

SR9011 also suppressed the expression of BMAL1 messenger RNA in HepG2 cells in a REV-ERB-a/b-dependent manner. Moreover, SR9011 inhibited the activity of the SCNclock, with reversible inhibition of circadian oscillations.