Nuclear Hormone Receptor 4A/NR4A Activator

Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.

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.

IP7e is a potent, brain-penetrant and orally active Nurr1 activator with an EC₅₀ value of 3.9 nM.

Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.

SR10098 is a benzimidazole-based Nurr1 activator with an EC₅₀ of 24 nM against full-length Nurr1. SR10098 does not directly bind to the ligand-binding domain of Nurr1, regulates transcription via a Nurr1-independent pathway, and exhibits no significant cytotoxicity. SR10098 can be used in studies of Nurr1-related diseases, such as Alzheimer's disease and Parkinson's disease.