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-155205
    GV150013X
    		Antagonist
    GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with Ki of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder.
    GV150013X
  • HY-150036
    Anthramycin
    		Antagonist
    Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice.
    Anthramycin
  • HY-117437
    Azintamide
    		Modulator
    Azintamide (Bilipurum) can be used for the research of psoriasis vulgaris, dyspepsia and other conditions.
    Azintamide
  • HY-118314
    CI-1015
    CI-1015 is a potent CCK-B receptor antagonist.
    CI-1015
  • HY-P2592
    Ro 23-7014
    Ro 23-7014 is an appetite suppressant. Ro 23-7014 is an analog of cholecystokinin (CCK-7).
    Ro 23-7014
  • HY-P1593
    Mini Gastrin I, human
    Mini Gastrin I, human is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
    Mini Gastrin I, human
  • HY-P2627
    CCK (27-33)
    CCK (27-33) is the C-terminal heptapeptide of cholecystokinin (CCK).
    CCK (27-33)
  • HY-160045
    AP1153 aptamer sodium
    		Chemical
    AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo.
    AP1153 aptamer sodium
  • 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-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-P5413
    [Lys3]-Bombesin
    [Lys3]-Bombesin is a biological active peptide. (PET (Positron Emission Tomography) imaging of [Lys3]-bombesin is able to detect gastrin-releasing peptide receptor (GRPR) positive prostate cancer. An immunoconjugate of [Lys3]-bombesin and corresponding monoclonal antibody can specifically induce (CD64)-dependent monocyte and neutrophil-mediated lysis of small cell carcinoma.)
    [Lys3]-Bombesin
  • HY-11076
    GI 181771
    		Agonist
    GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
    GI 181771
  • HY-123434
    PD-149164
    		Agonist
    PD-149164 is a potent agonist of cholecystokinin B (CCK-B) receptor, with IC50 values of 0.083 nM and 75 nM in binding assay to CCK-B and CCK-A.
    PD-149164
  • 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-P1710
    ARL 15849XX
    		Agonist
    ARL 15849XX is a cholecystokinin-8 (CCK-8) analog.
    ARL 15849XX
Cholecystokinin Receptor Isoform Comparison

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