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-120302
    PD 140376
    		Antagonist
    PD 140376 is a potent antagonist for the cholecystokininB/gastrin receptor, with Ki values of 0.18 nM and 0.21 nM in guinea-pig cortex and gastric gland membranes, respectively.
    PD 140376
  • HY-105226
    CI-988
    		Antagonist
    CI-988 (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 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects.
    CI-988
  • HY-106347
    Itriglumide
    		Antagonist
    Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC50 of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC50 of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity.
    Itriglumide
  • HY-P1800
    Caerulein, desulfated
    		Control
    Caerulein, desulfated is the desulfurated form of Caerulein. Caerulein is a decapeptide having the same five carboxyl-terminal amino acids as gastrin and cholecystokinin (CCK).
    Caerulein, desulfated
  • HY-105955
    FPL 14294
    FPL 14294 is a intranasally active anorectic agent and a cholecystokinin octapeptide (CCK) analog with enhanced metabolic stability. FPL 14294 induces satiety in many species and can be utilized in relevant research.
    FPL 14294
  • 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-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-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)
Cholecystokinin Receptor Isoform Comparison

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