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-111918
    A71378
    		Agonist
    A71378 is a selectivity CCK-A receptor agonist the IC50 values of 0.4 nM, 300 nM, and 1,200 nM for the pancreatic CCK-A, cortical CCK-B, and gastrin receptor, respectively. A71378 elicits pancreatic amylase secretion (EC50 = 0.16 nM) and ileal muscle contraction (EC50 = 3.7 nM).
    A71378
  • HY-129688
    Sut-8701
    Sut-8701 is a Cholecystokinin (HY-P2932) analog that effectively slows the degenerative process of Alzheimer's disease by protecting the integrity of cholinergic neurons in the nucleus basalis.
    Sut-8701
  • HY-177506
    FE100726
    		Agonist
    FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research.
    FE100726
  • HY-106231
    Gastrazole free acid
    		Inhibitor
    Gastrazole (JB95008) free acid is a gastrin receptor antagonist with activity against pancreatic cancer.
    Gastrazole free acid
  • HY-120381
    PD 136450
    		Antagonist
    PD 136450 (CAM 1189) is an antagonist for cholecystokinin 2 (CCK2). PD 136450 exhibits anti-secretory, anxiolytic and anti-ulcer activities, inhibits gastric acid secretion (IC50=1 mg/kg), and ameliorates the haemorrhagic lesions (IC50=4.7 mg/kg) in rats.
    PD 136450
  • HY-P5109
    Minigastrin
    Minigastrin is an acidic peptide. Minigastrin can be used to study peptidepeptide interaction.
    Minigastrin
  • HY-103354A
    Proglumide hemicalcium
    		Antagonist
    Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities.
    Proglumide hemicalcium
  • HY-11076
    GI 181771
    		Agonist
    GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
    GI 181771
  • HY-164634
    CLIK-148
    		Inhibitor
    CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.
    CLIK-148
  • HY-117828
    PF-04756956
    		Inhibitor
    PF-04756956 is a highly potent type 1 cholecystokinin receptor (CCK1R) agonist (EC50=0.47 nM). PF-04756956 is promising for research of obesity and related metabolic disorders.
    PF-04756956
  • HY-118546
    JNJ-17156516
    		Antagonist
    JNJ-17156516 is an orally active, potent, and selective cholecystokinin (CCK)1-receptor antagonist.
    JNJ-17156516
  • HY-169139
    Spiroglumide
    		Antagonist
    Spiroglumide (CR-2194) is a selective cholecystokinin B (CCKB) receptor antagonist.
    Spiroglumide
  • HY-109028
    Ceclazepide
    		Antagonist
    Ceclazepide (TR2-A), a CCK2R antagonist, is an orally active Mycobacterium abscessus inhibitor. Ceclazepide inhibits acid secretion in rats. Ceclazepide effectively suppresses the growth of M. abscessus wild-type strain and multiple subspecies. Ceclazepide inhibits M. abscessus growth within macrophages without causing harm.
    Ceclazepide
  • HY-117781
    GW-5823
    		Agonist
    GW-5823 is a selective CCK-AR agonist with an EC50 of 70 nM. GW-5823 can be studied in research on obesity.
    GW-5823
  • 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-125431
    LY 202769
    		Antagonist
    LY 202769 (Example 26) is a cholecystokinin (CCK) and gastrin receptor (gastrin receptor) antagonist. LY 202769 is applicable for the research of gastrointestinal diseases and central nervous system diseases.
    LY 202769
Cholecystokinin Receptor Isoform Comparison

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