Cholecystokinin Receptor Inhibitor

CCK-B Receptor Antagonist 2, compound 15b, is a potent and orally active Gastrin/CCK-B antagonist with an IC₅₀ value of 0.43 nM. CCK-B Receptor Antagonist 2 also inhibits gastrin/CCK-A activity with an IC₅₀ of 1.82 μM.

Gastrazole (JB95008) free acid is a gastrin receptor antagonist with activity against pancreatic cancer.

CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.

PF-04756956 is a highly potent type 1 cholecystokinin receptor (CCK1R) agonist (EC₅₀=0.47 nM). PF-04756956 is promising for research of obesity and related metabolic disorders.

PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models.

KSG-504 (anhydrous) is a CCK receptor antagonist. KSG-504 (anhydrous) inhibits the development of Ethionine-induced acute pancreatitis in rats and facilitates the regeneration of acinar cells.

CCK-A receptor inhibitor 1 is a cholecystokinin A (CCK-A) receptor inhibitor with a binging IC₅₀ of 340 nM.