1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Cholecystokinin Receptor

Cholecystokinin Receptor

CCK Receptor

Cholecystokinin receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin. Two types of functional membrane receptors, cholecystokinin A receptor (CCK-AR), located mainly on pancreatic acinar cells, and CCK-BR, mostly in the stomach and nervous system tissues, have been identified as the endogenous receptors of CCK. Both have high affinity for the sulfated CCK octapeptide (CCK-8), whereas only the CCK-BR has high affinity for gastrin.

CCK is a peptide hormone discovered in the small intestine. Together with secretin and gastrin, CCK constitutes the classical gut hormone triad. In addition to gallbladder contraction, CCK also regulates pancreatic enzyme secretion and growth, intestinal motility, satiety signalling and the inhibition of gastric acid secretion. CCK is also a transmitter in central and intestinal neurons.

Cholecystokinin Receptor Related Products (44):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-A0190
    Ceruletide
    Agonist 99.96%
    Ceruletide is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.
    Ceruletide
  • HY-P1097
    Gastrin I, human
    99.93%
    Gastrin I, human is the endogenous peptide produced in the stomach, and increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor.
    Gastrin I, human
  • HY-A0261
    Pentagastrin
    Activator 99.97%
    Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury..
    Pentagastrin
  • HY-106301
    Devazepide
    Antagonist 99.58%
    Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders.
    Devazepide
  • HY-P0093
    Sincalide
    99.26%
    Sincalide (Cholecystokinin octapeptide, CCK‐8) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK. CCK‐8 can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. CCK‐8 can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. CCK‐8 is a major bioactive segment of CCK that retains most of the biological activities of CCK.
    Sincalide
  • HY-105226B
    CI-988 hemihydrate
    Antagonist
    CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects.
    CI-988 hemihydrate
  • HY-160045
    AP1153 aptamer sodium
    Chemical
    AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo.
    AP1153 aptamer sodium
  • HY-118546
    JNJ-17156516
    Antagonist
    JNJ-17156516 is an orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist.
    JNJ-17156516
  • HY-P0093A
    Sincalide ammonium
    99.90%
    Sincalide ammonium (Cholecystokinin octapeptide ammonium, CCK-8 ammonium) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. Sincalide ammonium is a major bioactive segment of CCK that retains most of the biological activities of CCK. CCK‐8 can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. Sincalide ammonium can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. Sincalide ammonium is a major bioactive segment of CCK that retains most of the biological activities of CCK.
    Sincalide ammonium
  • HY-14850
    Sograzepide
    Antagonist 98.35%
    Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
    Sograzepide
  • HY-125556
    Tetragastrin
    Agonist 99.73%
    Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. Tetragastrin can stimulate gastric secretion. Tetragastrin is a Cholecystokinin (CCK-4) receptor agonist. Gastric mucosal protection.
    Tetragastrin
  • HY-106840
    L-365260
    Antagonist 99.93%
    L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.
    L-365260
  • HY-103354
    Proglumide sodium
    Antagonist 99.85%
    Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.
    Proglumide sodium
  • HY-B1330
    Proglumide
    Antagonist 99.74%
    Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities.
    Proglumide
  • HY-11077
    SR 146131
    Agonist 98.81%
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
    SR 146131
  • HY-17617
    Nastorazepide
    Antagonist 99.95%
    Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
    Nastorazepide
  • HY-P1096
    A71623
    Agonist 99.90%
    A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively.
    A71623
  • HY-B1439B
    Lorglumide sodium salt
    Antagonist 99.71%
    Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.
    Lorglumide sodium salt
  • HY-128878
    Dexloxiglumide
    Antagonist 98.25%
    Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8).
    Dexloxiglumide
  • HY-P2416
    Gastrin I, rat
    Activator 99.29%
    Gastrin I, rat (Rat Gastrin-17) is a peptide hormone, can stimulate gastric acid secretion potently.
    Gastrin I, rat