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-P1806
    Gastrin I (1-14), human
    Gastrin I (1-14), human is 1-14 fragment of human gastrin I peptide. Gastrin I is an endogenous, gastrointestinal peptide hormone. Gastrin is the major hormonal regulator of gastric acid secretion.
    Gastrin I (1-14), human
  • 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-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-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-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-14575
    Nastorazepide hemicalcium
    		Antagonist
    Nastorazepide (Z-360) hemicalcium, selective, orally available, 1,5-benzodiazepine derivative, is a gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antitumor activity.
    Nastorazepide hemicalcium
  • HY-158722
    Caerulein acetate
    		Agonist
    Caerulein acetate is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide acetate is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.
    Caerulein acetate
  • 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
  • HY-P2638
    Cholecystokinin (27-32)-amide
    		Antagonist
    Cholecystokinin (27-32)-amide (CCK-27-32-NH2) is a potent cholecystokinin receptor CCK receptor antagonist.
    Cholecystokinin (27-32)-amide
  • HY-118665
    L-736380
    		Antagonist
    L-736380 is a high affinity CCK-B (cholecystokinin B receptor) receptor antagonist, with IC50 values of 0.054 nM and 400 nM for CCK-B and CCK-A, respectively. L-736380 dose-dependently inhibits gastric acid secretion in anesthetized rats (ID50, 0.064 mg/kg) and ex vivo binding of [125I]CCK-8S in BKTO mice brain membranes (ED50, 1.7 mg/kg).
    L-736380
  • HY-P1994
    JMV 167
    		Antagonist
    JMV 167 is antagonist of peripheral cholecystokinin receptor (CKK), with an IC50 of 500 nM.
    JMV 167
  • HY-162070
    CCK antagonist 1
    		Antagonist 99.96%
    CCK antagonist 1 (compound 3d) is a CCK antagonist with IC50s of 1.1 μM and 4 μM for CCK1 and CCK2, respectively. CCK antagonist 1 can be used for research of cancer and mental disease.
    CCK antagonist 1
Cholecystokinin Receptor Isoform Comparison

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