GSK4112 is a selective Rev-Erbα agonist (EC50=250 nM). It induces circadian clock phase shifts in isolated primary lung fibroblasts as well as in lung slices (10 µM). GSK4112 showed an inhibitory effect on the amplitude of circadian oscillations and caused an arrhythmic expression of canonical...
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GSK4112 is a selective Rev-Erbα agonist (EC50=250 nM). It induces circadian clock phase shifts in isolated primary lung fibroblasts as well as in lung slices (10 µM). GSK4112 showed an inhibitory effect on the amplitude of circadian oscillations and caused an arrhythmic expression of canonical clock genes. In murine RAW264 macrophages it suppressed inflammatory functions via repressing Ccl2 expression. It protected RANKL-induced bone loss via inhibition of osteoclast differentiation in vivo
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