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-B1439
    Lorglumide
    		Antagonist
    Lorglumide (CR-1409) is a potent cholecystokinin (CCK) receptor antagonist. Lorglumide can be used in the research of pancreatic secretion and growth.
    Lorglumide
  • HY-177508
    BC264
    		Agonist
    BC264 is a highly potent and selective CCK-B agonist that crosses the blood-brain barrier. BC264 increases dopamine in the nucleus accumbens and facilitates motivation and attention in rats.
    BC264
  • HY-P2165
    N-acetyl CCK-(26-30) amide
    		Antagonist
    N-acetyl CCK-(26-30) amide (CCK-(26-30) (sulfated)) is a cholecystokinin (CCK) receptor antagonist.
    N-acetyl CCK-(26-30) amide
  • 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-116260
    RP-69758
    		Antagonist
    RP-69758 is a potent and selective non-peptide cholecystokinin-B (CCKB)/gastrin receptor antagonist. RP-69758 exhibits >200-fold selectivity for CCKB over CCKA receptors. RP-69758 antagonizes CCK-8-induced neuronal firing in rat hippocampal slices. RP-69758 inhibits Pentagastrin (HY-A0261)-induced gastric acid secretion in the rat. RP-69758 can be used for neurological disorders and gastrointestinal disease research.
    RP-69758
  • HY-103285
    GRP (porcine)
    		Activator
    GRP (porcine) (Porcine gastrin-releasing peptide 27) is the putative mammalian analog of Bombesin (HY-P0195). GRP (porcine) activates the release of a number of gastroenteropancreatic (GEP) peptides into the peripheral circulation. GRP (porcine) stimulates gastrin release and exocrine pancreatic secretion. GRP (porcine) is a useful marker of neuroendocrine differentiation in many tumors.
    GRP (porcine)
  • HY-P2121
    JMV 176
    		Agonist
    Jmv 176 is a CCK agonist when first given and becomes a cholecystokinin antagonist after 3-4 hours.
    JMV 176
  • HY-U00363
    CHEMBL333994
    		Antagonist
    CHEMBL333994 (FK-480) 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.
    CHEMBL333994
  • HY-106356
    GV-150013
    		Antagonist
    GV-150013 is a selective CCK-B receptor antagonist. GV-150013 has sleep aid effect.
    GV-150013
  • HY-P1994
    JMV 167
    		Antagonist
    JMV 167 is antagonist of peripheral cholecystokinin receptor (CKK), with an IC50 of 500 nM.
    JMV 167
  • HY-113896
    U-67827E
    		Agonist
    U-67827E is a cholecystokinin (CCK) agonist that decreases food intake over a prolonged period of time in baboons. U-67827E may affect the latency to food by inhibiting the movement of food in the stomach and magnifying a gastric distention signal.
    U-67827E
  • HY-125692
    L-740093
    		Antagonist
    L-740093 is a potent cholecystokinin-B receptor antagonist. L-740093 has excellent central nervous system (CNS) penetration.
    L-740093
  • HY-121278
    Benzotript
    		Antagonist
    Benzotript (Benzotriptum) is a cholecystokinin-receptor (CCK) and gastrin receptor antagonist. Benzotript shows antiproliferative effects in human colon carcinoma cell lines.
    Benzotript
  • HY-120862
    L 368935
    		Antagonist
    L 368935 is a cholecystokinin B receptor (CCKB receptor) antagonist. L 368935 is a brain-penetrant and centrally active compound.
    L 368935
  • 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-177509
    BBL454
    		Agonist
    BBL454 (Compound 43) is a Cholecystokinin 2B (CCK2B) receptor agonist. BBL454 induces hyperactivity and improves memory in rat models while it has weak activity on the peripheral CCK2 receptor and no anxiogenic activity. BBL454 increases gastric acid output in anesthetised rat models. BBL454 can be used for diabetes research.
    BBL454
  • 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
Cholecystokinin Receptor Isoform Comparison

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