CAS: 1516896-09-5

PDE10-IN-1 (SEP-0372814) is used for treating CNS and metabolic disorders.

PDE10-IN-1

PDE10-IN-1 is a peptide with the amino acid sequence of GGRDYGGLPPG. It is an activator of PDE10, which belongs to the family of phosphodiesterases. The inhibition of PDE10 in the brain has been shown to have antidepressant effects in mice and rats. This peptide has been shown to be a potent inhibitor of protein interactions, with IC50 values ranging from 1 μM to 10 μM for a number of proteins including TNF-α receptor (IC50 = 2 μM), CD4 receptor (IC50 = 1 μM), and CX3CR1 receptor (IC50 = 0.5 μM). In addition, PDE10-IN-1 has been shown to be a ligand for the dopamine D2 receptor and may function as an antagonist or agonist depending on its binding affinity.