RORα Activator

6'''-Feruloylspinosin is an orally active RORα activator that crosses the blood-brain barrier, with a K_d of 0.308 μM, and is found in natural sources. 6'''-Feruloylspinosin modulates AMPK and mTOR phosphorylation. 6'''-Feruloylspinosin promotes autophagy through the AMPK/mTOR signaling pathway, inhibits GSK3β phosphorylation at Tyr216, and activates the PGC-1α/Nrf2/HO-1 pathway. 6'''-Feruloylspinosin regulates neurotransmitter levels, enhances mRNA expression of GABA_A α1, α5, and GABA_B R1 receptor subunits, increases brain 5-HT and GABA, restores melatonin levels, and ameliorates anxiety-like behaviors. 6'''-Feruloylspinosin regulates oxidative stress homeostasis, inhibits mitochondrial dysfunction, decreases MDA while increasing GSH. 6'''-Feruloylspinosin can be used for research on Alzheimer's disease, acute myocardial infarction, heart failure with insomnia, and insomnia.

CM002 is a circadian clock activator. CM002 inhibits the lineage commitment and terminal differentiation of preadipocytes by activating the circadian clock, thereby blocking the adipogenesis process driven by Wnt signaling-mediated transcriptional induction. CM002 attenuates lipid storage in a clock-dependent manner via inhibition of the lipogenic program in mature adipocytes. CM002 enhances circadian clock output across various adipose depots in both lean and obese mice through BMAL1/CLOCK-dependent metabolic reprogramming, inhibits adipocyte development and hypertrophy, and improves insulin sensitivity. CM002 can be used in research on obesity and type 2 diabetes.