cck2

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

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.

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.

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

CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in mice when administered at doses up to 1 uMol/kg.

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.

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].