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. Author manuscript; available in PMC: 2011 Nov 19.

Published in final edited form as: ACS Chem Biol. 2010 Nov 19;5(11):1029–1034. doi: 10.1021/cb100223d

SR1078 activates ROR target gene transcription both in vitro and in vivo. HepG2 cells expressing natural levels of RORα and RORγ were treated with 10 μM SR1078 for 24h followed by assessment of either FGF21 (A) or G6Pase (B) gene expression. The expression of both of these ROR target genes was stimulated by the ROR agonist. C) Analysis of plasma levels of SR1078 following i.p. injection of the compound at a dose of 10 mg/kg in mice. D and E) Levels of expression of FGF21 (D) and G6Pase (E) mRNA 2h following injection (i.p. 10 mg/kg) of SR1078.

SR1078 activates ROR target gene transcription both in vitro and in vivo. HepG2 cells expressing natural levels of RORα and RORγ were treated with 10 μM SR1078 for 24h followed by assessment of either FGF21 (A) or G6Pase (B) gene expression. The expression of both of these ROR target genes was stimulated by the ROR agonist. C) Analysis of plasma levels of SR1078 following i.p. injection of the compound at a dose of 10 mg/kg in mice. D and E) Levels of expression of FGF21 (D) and G6Pase (E) mRNA 2h following injection (i.p. 10 mg/kg) of SR1078.