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-129810
    PD 135158
    		Antagonist
    PD 135158 (CAM 1028) is a selective CCKB receptor antagonist with an IC50 of 2.8 nM against mouse cortex CCKB. PD 135158 shows anxiolytic activity.
    PD 135158
  • HY-103357A
    LY262691
    		Antagonist
    LY262691 is a selective CCK-B antagonist with antipsychotic properties. LY262691 decreases the number of spontaneously active A9 and A10 dopamine cells and can be utilized in antipsychotic research.
    LY262691
  • HY-19261
    T-0632
    		Antagonist
    T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
    T-0632
  • 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-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-P2677
    CCK (26-31) sulfated
    CCK (26-31) (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) sulfated
  • HY-U00363
    CHEMBL333994
    		Antagonist
    CHEMBL333994 is a potent and orally effective Cholecystokinin A (CCK-A) antagonist, with an IC50 of 0.67 nM.
    CHEMBL333994
  • HY-111313
    JNJ-26070109
    		Antagonist
    JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease.
    JNJ-26070109
  • HY-106356
    GV-150013
    		Antagonist
    GV-150013 is a selective CCK-B receptor antagonist. GV-150013 has sleep aid effect.
    GV-150013
  • 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-P3446A
    Big Gastrin I (human) TFA
    Big Gastrin I, human (TFA) is a gastrointestinal hormone consisting of 34 amino acids. Big Gastrin I, human (TFA) can be used as a potential substance for the study of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurological diseases or cardiovascular diseases.
    Big Gastrin I (human) TFA
  • 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
Cholecystokinin Receptor Isoform Comparison

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