2. GPCR/G Protein
    Neuronal Signaling
  3. 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 (30):

Cat. No. Product Name Effect Purity
  • 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-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-A0261
    Pentagastrin Activator 99.97%
    Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM[1]. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury[2].
  • HY-106301
    Devazepide Antagonist 98.90%
    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-14850
    Sograzepide Antagonist 98.51%
    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[1]. 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[2].
  • HY-P1096
    A71623 Agonist
    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[1].
  • HY-125556
    Tetragastrin Agonist
    Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. Tetragastrin can stimulate gastric secretion[1]. Tetragastrin is a Cholecystokinin (CCK-4) receptor agonist[2]. Gastric mucosal protection[3].
  • HY-103357
    LY288513 Antagonist
    LY288513, a selective non-peptide CCK-B receptor antagonist with an IC50 value of 16 nM. LY288513 possesses both anxiolytic and antipsychotic potential[1][2][3].
  • HY-B1439B
    Lorglumide sodium salt Antagonist
    Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist[1].
  • HY-B2154
    Loxiglumide Antagonist
    Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
  • HY-128878
    Dexloxiglumide Antagonist 98.25%
    Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist[1]. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8)[2].
  • 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.
  • HY-11077
    SR 146131 Agonist 98.02%
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
  • HY-101764
    Lintitript Antagonist
    Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin[1][2][3].
  • HY-129357
    CCK-B Receptor Antagonist 2 Inhibitor 98.84%
    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[1].
  • HY-U00360
    CCK-B Receptor Antagonist 1 Antagonist 99.04%
    CCK-B Receptor Antagonist 1 is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
  • HY-103354
    Proglumide sodium Antagonist 99.63%
    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-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[1][2][3][4][5].
  • HY-P1593A
    Mini Gastrin I, human TFA 98.08%
    Mini Gastrin I, human (TFA) is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
  • 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].