cck1

Lintitript (SR 27897) is a selective CCK1 antagonist with an EC50 of 6 nM for CCK1 and 200 nM for CCK2, and a Ki value of 0.2 nM for CCK1.

CCK1-specific peptide substrate is a bioactive peptide. [The peptide sequence is based on Ser7-phosphorylated rabbit muscle glycogen synthase.] It serves as a peptide substrate for casein kinase I (CK1), which phosphorylates Ser10. In vivo, Ser7 is phosphorylated by PKA.

Devazepide is a competitive, selective, orally available non-peptide CCK1 (cholecystokinin 1) receptor antagonist that inhibits bladder cancer cell proliferation and migration while inducing apoptosis and cell cycle arrest.

ZP3022 is a dual agonist targeting the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor. It selectively enhances cAMP accumulation or ERK phosphorylation in HEK293 cells with GLP-1R or CCK2 receptor expression, compared to ERK phosphorylation in cells with the CCK1 receptor (EC50s: 0.02, 10.3, and >1,000 nM for human receptors, respectively). At 40 nM, ZP3022 promotes proliferation of rat neonatal β-cells in vitro. It also boosts glucose-induced insulin secretion (GSIS) in rat pancreatic islets at 10 and 100 nM concentrations and decreases body weight in rats at 40 nmol/kg doses twice daily. Administered at 100 nmol/kg daily, ZP3022 enhances β-cell and total pancreatic mass and improves glucose tolerance in db/db mice, while reducing food intake but not body weight in these mice.

CI-988 hemihydrate (PD134308) is a potent and selective orally active CCK2R (cholecystokinin 2 receptor) antagonist, with an IC50 of 1.7 nM for mouse cortical CCK2. It is over 1600 times more selective for CCK2 than for CCK1 receptors. CI-988 hemihydrate exhibits anxiolytic and antitumor properties.

CCK2 (CCK-B) receptor antagonist

VL-0395 is an antagonist of CCK1 receptor.

Enterostatin (rat), a procolipase activation peptide with oral activity, selectively diminishes fat consumption and lowers serum cholesterol through a CCK1 receptor-dependent mechanism [1] [2].