2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
SR9009 is an agonist of REV-ERB with IC50 = 670 nM for REV-ERBα and IC50 = 800 nM for REV-ERBβ.
in vitro: SR9009 dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD) - REV-ERB ligand binding domain (LBD) α or β and a Gal4-responsive luciferase reporter. SR9009 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9009 IC50=710 nM). SR9009 suppresses the expression of BMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner.
in vivo: SR9009 are synthetic REV-ERB agonists with activity. SR9009 also inhibits the activity of the SCN clock, with reversible inhibition of circadian oscillations in SCN explants cultured from the Per2:luc reporter mouse.
