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-169139
    Spiroglumide
    		Antagonist
    Spiroglumide (CR-2194) is a selective cholecystokinin B (CCKB) receptor antagonist.
    Spiroglumide
  • HY-P1710
    ARL 15849XX
    		Agonist
    ARL 15849XX is a cholecystokinin-8 (CCK-8) analog.
    ARL 15849XX
  • HY-14575
    Nastorazepide hemicalcium
    		Antagonist
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
    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-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-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-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-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-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
Cholecystokinin Receptor Isoform Comparison

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