insulin levels modulator

Insulin level regulators can be used to treat diabetes.

PPARγmodulator-2 (Compound (R)-2n) is a reversible modulator of PPARγ, inhibiting the PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. It helps lower blood glucose levels, improves glucose tolerance and insulin sensitivity, and demonstrates antidiabetic activity in db/db mouse models.

GLP-1R modulator-1 (Compound 384) is a potent and orally active selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). It activates G protein-coupled signaling, leading to increased intracellular cAMP levels, enhanced insulin secretion, delayed gastric emptying, and reduced appetite. GLP-1R modulator-1 holds potential for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

YGT-31 is a PPARγ modulator with an IC50 of 1.72 μM and a Ki of 0.62 μM. It diminishes blood glucose levels and enhances insulin sensitivity in a type 2 diabetes model in db/db mice by inhibiting CDK5-mediated phosphorylation of PPARγ-Ser273. Additionally, YGT-31 exhibits anti-steatotic effects in a mouse model of non-alcoholic fatty liver disease (NAFLD).