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

Cholecystokinin Receptor

CCK Receptor

Cholecystokinin Receptor

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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 Isoform Specific Products:

Cholecystokinin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-A0190
    Caerulein
    		Agonist 99.96%
    Caerulein is a decapeptide and a potent cholecystokinin receptor agonist. Caerulein is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.
    Caerulein
  • 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-P2671
    [Leu15]-Gastrin I (human)
    		99.98%
    [Leu15]-Gastrin I (human) is a Gastrin I, human (HY-P1097) peptide hormone derivative, which is trophic for normal gastrointestinal epithelium. Gastrin stimulates growth of gastric adenocarcinoma (gastric cancer) through G-protein-coupled receptor called the cholecystokinin (CCK) or cholecystokinin-B receptors (CCK-BR) that are overexpressed in this malignancy. [Leu15]-Gastrin I (human) is promising for research of gastric cancer.
    [Leu15]-Gastrin I (human)
  • HY-P0093
    Sincalide
    		99.30%
    Sincalide (Cholecystokinin octapeptide, CCK-8) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. Sincalide is a major bioactive segment of CCK that retains most of the biological activities of CCK. Sincalide can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. Sincalide can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. Sincalide is a major bioactive segment of CCK that retains most of the biological activities of CCK.
    Sincalide
  • HY-A0261
    Pentagastrin
    		Agonist 99.97%
    Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCKB) receptor agonist with an EC50 value of 11 nM. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury.
    Pentagastrin
  • HY-P11540
    CCKBR agonist-1
    		Agonist 98.48%
    CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC50 of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC50 of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease.
    CCKBR agonist-1
  • HY-179721
    CCKBR agonist-2
    		Agonist 99.81%
    CCKBR agonist-2 (Compound z-44) is a Gi-preferring CCKBR agonist. CCKBR agonist-2 effectively activates the CCKBR-Gi signaling pathway (EC50 = 0.27 nM), but has almost no activity on Gq and Gs signaling pathways. CCKBR agonist-2 shows no significant protective effect in the mouse Alzheimer's disease model, proving that the simple activation of the Gi signal pathway does not play a dominant role in the improvement of cognitive function.
    CCKBR agonist-2
  • HY-186122
    CCK2R agonist-1
    		Agonist
    CCK2R agonist-1 (Compound 2S) is a CCK2R agonist, with an IC50 of 48 nM against wild-type CCK-2R and an IC50 of 450 nM against mutant CCK-2R (N353L). CCK2R agonist-1 stimulates the production of inositol phosphate. The changes in pH and HDC induced by CCK2R agonist-1 in mice are comparable to those induced by the full-length peptide agonist Gastrin. CCK2R agonist-1 can be used in studies of gastric diseases and pain.
    CCK2R agonist-1
  • HY-106301
    Devazepide
    		Antagonist 99.55%
    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-106840
    L-365260
    		Antagonist 99.85%
    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-11077
    SR 146131
    		Agonist 98.23%
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
    SR 146131
  • HY-P2932
    Cholecystokinin
    		98.16%
    Cholecystokinin is a peptide hormone. Cholecystokinin, as a hunger suppressant, inhibits food intake and stimulates the digestion of fat and protein. Cholecystokinin can be used for the research of gastrointestinal system.
    Cholecystokinin
  • HY-P0196
    Cholecystokinin Octapeptide, desulfated
    		99.45%
    Cholecystokinin Octapeptide, desulfated (CCK Octapeptide, desulfated) is a synthetic desulfated Cholecystokinin octapeptide (HY-P0093).
    Cholecystokinin Octapeptide, desulfated
  • HY-125556
    Tetragastrin
    		Agonist 99.89%
    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-14850
    Sograzepide
    		Antagonist 98.04%
    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-B1439B
    Lorglumide sodium
    		Antagonist 99.19%
    Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.
    Lorglumide sodium
  • HY-P1096
    A71623
    		Agonist 99.34%
    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-P0093A
    Sincalide ammonium
    		99.21%
    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-B1330
    Proglumide
    		Antagonist 99.84%
    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-128878
    Dexloxiglumide
    		Antagonist 98.25%
    Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors.
    Dexloxiglumide
Cholecystokinin Receptor Isoform Comparison

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