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

Cholecystokinin 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 (54):

Cat. No. Product Name Effect Purity
  • 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[1][2][3].
  • HY-A0190
    Ceruletide Agonist
    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[1].
  • 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[1].
  • 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[1].[2].
  • 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.
  • HY-117896
    SC-50605 Inhibitor
    PD-135666 is a dipeptide that inhibits the cholecystokinin B (CCK B) receptor more than the CCK A receptor. PD-135666 binds to CCK B receptors with an IC50 of 0.1 nM in mouse cerebral cortex, whereas its enantiomer PD-140548 preferentially binds to CCK A receptors with an IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models[1].
  • HY-P1710
    ARL 15849XX Agonist
    ARL 15849XX is a cholecystokinin-8 (CCK-8) analog[1].
  • HY-116576
    LY219057 Antagonist
    LY219057 is a potent antagonist of cholecystokinin octapeptide (CCK-8), with the ID50 of 287.5 nM[1][2].
  • 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[1][2][3][4][5].
  • HY-19445
    Gastrazole Antagonist
    Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer[1][2].
  • HY-155205
    GV150013X Antagonist
    GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with Ki of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder[1].
  • HY-150036
    Anthramycin Antagonist
    Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice[1][2][3].
  • HY-P0093R
    Sincalide (Standard)
    Sincalide (Standard) is the analytical standard of Sincalide. This product is intended for research and analytical applications. 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[1][2][3].
  • HY-U00387
    CCK-A receptor inhibitor 1 Inhibitor
    CCK-A receptor inhibitor 1 is a cholecystokinin A (CCK-A) receptor inhibitor with a binging IC50 of 340 nM.
  • HY-P1593
    Mini Gastrin I, human
    Mini Gastrin I, human is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
  • 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[1].
  • 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[1][2][3].
  • HY-106301R
    Devazepide (Standard) Antagonist
    Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. 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[1].
  • HY-103354A
    Proglumide hemicalcium Antagonist
    Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities[1][2][3][4][5].
  • HY-11076
    GI 181771 Agonist
    GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.