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-P1097F
    Biotin-Gastrin-1, human (1-17)
    		99.02%
    Biotin-Gastrin-1, human (1-17) is a biological active peptide. (Biotin-labeled HY-P1097)
    Biotin-Gastrin-1, human (1-17)
  • 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-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-B1439B
    Lorglumide sodium salt
    		Antagonist 99.19%
    Lorglumide sodium salt (CR-1409 sodium salt) is a potent cholecystokinin (CCK) receptor antagonist.
    Lorglumide sodium salt
  • HY-17617
    Nastorazepide
    		Antagonist 99.95%
    Nastorazepide (Z-360), selective, orally available, 1,5-benzodiazepine derivative, is a gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antitumor activity.
    Nastorazepide
  • HY-B2154
    Loxiglumide
    		Antagonist ≥98.0%
    Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
    Loxiglumide
  • HY-P2416
    Gastrin I, rat
    		Activator 99.83%
    Gastrin I, rat (Rat Gastrin-17) is a peptide hormone, can stimulate gastric acid secretion potently.
    Gastrin I, rat
  • HY-P0196A
    Cholecystokinin Octapeptide, desulfated TFA
    Cholecystokinin Octapeptide, desulfated TFA is a synthetic desulfated octapeptides of Cholecystokinin (CCK).
    Cholecystokinin Octapeptide, desulfated TFA
  • HY-106840A
    L-365260 hemihydrate
    		Antagonist 99.75%
    L-365260 hemihydrate 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 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors.
    L-365260 hemihydrate
  • HY-148656
    PNB-001
    		Antagonist 99.65%
    PNB-001 is an orally active CCK2 selective ligand and antagonist. PNB-001 has anti-inflammatory and analgesic activities.
    PNB-001
  • HY-U00360
    (Rac)-Sograzepide
    		Antagonist 98.98%
    (Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
    (Rac)-Sograzepide
  • 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-105257
    Pranazepide
    		Antagonist 99.81%
    Pranazepide (FR120480) is a cholecystokinin-A receptor antagonist.
    Pranazepide
  • 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.
    CCK-B Receptor Antagonist 2
  • HY-P1593A
    Mini Gastrin I, human TFA
    		98.13%
    Mini Gastrin I, human (TFA) is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
    Mini Gastrin I, human TFA
  • HY-P2932A
    Cholecystokinin-33 free acid
    Cholecystokinin-33 free acid is an analogue of Cholecystokinin (HY-P2932). C-terminal amidation is important for binding of Cholecystokinin to its receptors, and removing the amide group would decrease Cholecystokinin activity. Cholecystokinin-33 free acid can be used to study C-terminal amidation of Cholecystokinin-33.
    Cholecystokinin-33 free acid
  • HY-U00062
    Tarazepide
    		Antagonist
    Tarazepide is a potent and specific CCK-A receptor antagonist.
    Tarazepide
  • HY-101352
    LY 225910
    		Antagonist 98.92%
    LY 225910 is a selective antagonist for cholecystokinin receptor (CCK2 receptor), which affects the excitatory response to morphine, and leads to morphine sensitization.
    LY 225910
  • HY-A0261A
    Pentagastrin meglumine
    		Agonist
    Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury..
    Pentagastrin meglumine
  • 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.
    Gastrazole
Cholecystokinin Receptor Isoform Comparison

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