cck2

Itriglumide (CR-2945) is a cholecystokinin (CCK)-2 receptor antagonist with antisecretory and antiulcerogenic properties.

Gastrin I, human (Gastrin I (human)) is an endogenous peptide produced in the stomach that increases pepsinogen and acid secretion via the CCK2 receptor in the rat.

Gastrin I (human) acetate (Gastrin-17 acetate) is the endogenous peptide produced in the stomach, and increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor.

Nastorazepide (Z-360) is a selective, orally available antagonist of the gastrin/cholecystokinin 2 (CCK-2) receptor with potential antineoplastic activity.

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

CCK2 (CCK-B) receptor antagonist

SGC-CK2-2 is an innovative and potent cell-active probe capable of inhibiting CK2/CSNK2.

SGC-CK2-1 is a highly specific inhibitor of CK2, a inducer of insulin production and secretion in pancreatic β-cells, and can be used in the study of neurodegenerative diseases.

HDAC/CK2-IN-1 (compound 38) acts as an inhibitor of HDAC1 (IC 50 = 1.46 μM), HDAC6 (IC 50 = 0.66 μM), and CK2 (IC 50 = 3.67 μM). It demonstrates promising antiproliferative effects on various cell lines, including Jurkat, MCF-7, HCT-116, and HL-60.

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.

GV150013 is an antagonist of cholecystokinin-2 (CCK2) receptor.

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.

FE101120 is a non-peptidic CCK2 receptor agonist. It is utilized in diabetes research.

FE100726 (Compound 39) is a cholecystokinin 2 (CCK2) receptor agonist with excellent binding affinity for the CCK2 receptor. It is capable of inducing gastric acid secretion in anesthetized rat models and has applications in diabetes research.

BBL454 (Compound 43) is an agonist of the cholecystokinin 2B (CCK2B) receptor. It induces hyperactivity and enhances memory in rat models, while showing weak activity on peripheral CCK2 receptors and no anxiogenic effects. In anesthetized rat models, BBL454 increases gastric acid secretion. It is applicable to diabetes research.

LY 225910 is a CCK2 receptor antagonist.

Selective CCK2 receptor antagonist

PD 135158 is a CCK2 receptor antagonist.

Gastrazole is a CCK2 receptor antagonist potentially. It also used for the treatment of pancreatic cancer.

Gastrazole, a CCK2 receptor antagonist, is used potentially for the treatment of pancreatic cancer.

JNJ-26070109, an antagonist of cholecystokinin CCK2 receptor, inhibits gastric acid secretion and prevents omeprazole-induced acid rebound in the rat.

PNB-001 is an orally active, CCK2-selective ligand and antagonist with anti-inflammatory and analgesic activities [1].