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-P3650
    Cholecystokinin (1-21)
    Cholecystokinin (1-21) (CCK-1-21) is a cholecystokinin (CCK) fragment. Cholecystokinin (1-21) stimulates lipolysis in human adipose tissue.
    Cholecystokinin (1-21)
  • HY-P2678
    CCK (26-31) non-sulfated
    		Agonist
    CCK (26-31) (non-sulfated) is the N-terminal fragment of CCK, a peptide hormone found in the gut and brain that stimulates digestion, regulates satiety, and is associated with anxiety. CCK (26-31) is also less active in non-sulfated than in sulfated form.
    CCK (26-31) non-sulfated
  • HY-103357
    LY288513
    		Antagonist
    LY288513 is a selective non-peptide CCK-B receptor antagonist with an IC50 value of 16 nM. LY288513 produces an anxiolytic-like action in mice.
    LY288513
  • HY-P1988
    JMV 179
    		Antagonist
    JMV 179, a peptide closely related to CCK, is a cholecystokinin receptor (CKK) antagonist, with an IC50 of 30 nM.
    JMV 179
  • HY-117839
    PD-135666
    		Inhibitor
    PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models.
    PD-135666
  • HY-P3652
    Cholecystokinin-33 (swine)
    		Agonist
    Cholecystokinin-33 (swine) is a cholecystokinin (CCK) fragment. Cholecystokinin-33 (swine) can reduce food intake and gallbladder contraction.
    Cholecystokinin-33 (swine)
  • HY-U00363A
    (rac)-CHEMBL333994
    		Control
    (rac)-CHEMBL333994 is the racemate of CHEMBL333994 (HY-U00363). CHEMBL333994 is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC50 of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis.
    (rac)-CHEMBL333994
  • HY-P1994A
    JMV 170
    		Agonist
    JMV 170, a CCK derivative, is a selective CCK-B agonist. JMV 170 binds to the CCK-B receptor with a 10-fold higher affinity than to the CCK-A receptor. JMV 170 shows contractile effects on pig smooth muscle cells with an EC50 of 9 pmol/L.
    JMV 170
  • HY-122336
    Asperlicin D
    		Antagonist
    Asperlicin D is a asperlicin productionfrom Aspergillus alliaceus strain (ATCC 20656).
    Asperlicin D
  • HY-125610
    DA-3934
    		Antagonist
    DA-3934 is a cholecystokinin (CCK)-B receptor antagonist. DA-3934 inhibits Pentagastrin (HY-A0261)-induced gastric acid secretion in rats.
    DA-3934
  • HY-103354R
    Proglumide sodium (Standard)
    		Antagonist
    Proglumide (sodium) (Standard) is the analytical standard of Proglumide (sodium). This product is intended for research and analytical applications. 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 (Standard)
  • HY-118904
    VL-0395
    		Antagonist
    VL-0395 is a CCK1 selective antagonist with IC50 of 0.197 μM for CCK1 in rat pancreatic acinar cells.
    VL-0395
  • HY-128878R
    Dexloxiglumide (Standard)
    		Antagonist
    Dexloxiglumide (Standard) is the analytical standard of Dexloxiglumide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-129759
    KSG-504 anhydrous
    		Inhibitor
    KSG-504 (anhydrous) is a CCK receptor antagonist. KSG-504 (anhydrous) inhibits the development of Ethionine-induced acute pancreatitis in rats and facilitates the regeneration of acinar cells.
    KSG-504 anhydrous
  • 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.
    Devazepide (Standard)
  • HY-123434
    PD-149164
    		Agonist
    PD-149164 is a potent agonist of cholecystokinin B (CCK-B) receptor, with IC50 values of 0.083 nM and 75 nM in binding assay to CCK-B and CCK-A.
    PD-149164
  • HY-B1330R
    Proglumide (Standard)
    		Antagonist
    Proglumide (Standard) is the analytical standard of Proglumide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-129516
    A-70874
    		Agonist
    A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (30-33) (CCK-4). A-70874 is an agonist that stimulates pancreatic amylase release and a partial agonist that stimulates pancreatic phosphoinositide decomposition. A-70874 has an IC50 of 4.9 nM for the guinea pig pancreatic CCK receptor. Cholecystokinin (CCK) receptors are divided into CCK-A (digestive tract) and CCK-B (brain). A-70874 has an affinity of 1.6 μM for the CCK-B/gastrin receptor.
    A-70874
  • HY-101764R
    Lintitript (Standard)
    		Antagonist
    Lintitript (Standard) (SR 27897 (Standard)) is the analytical standard of Lintitript (HY-101764). This product is intended for research and analytical applications. 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.
    Lintitript (Standard)
  • HY-119127
    TP-680
    		Antagonist
    TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCKA receptors (IC50=1.2 nM) than to rat brain CCKB receptors (IC50=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases.
    TP-680
Cholecystokinin Receptor Isoform Comparison

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