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-128878
    Dexloxiglumide
    		Antagonist 98.25%
    Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors.
    Dexloxiglumide
  • HY-P2416
    Gastrin I, rat
    		Activator 99.49%
    Gastrin I, rat (Rat Gastrin-17) is a peptide hormone, can stimulate gastric acid secretion potently.
    Gastrin I, rat
  • HY-P1097F
    Biotin-Gastrin-1, human (1-17)
    		99.18%
    Biotin-Gastrin-1, human (1-17) is a biological active peptide. (Biotin-labeled HY-P1097)
    Biotin-Gastrin-1, human (1-17)
  • HY-103354
    Proglumide sodium
    		Antagonist 99.58%
    Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.
    Proglumide sodium
  • HY-101764
    Lintitript
    		Antagonist 99.58%
    Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin.
    Lintitript
  • HY-17617
    Nastorazepide
    		Antagonist 99.95%
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide
  • HY-B2154
    Loxiglumide
    		Antagonist 98.0%
    Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.
    Loxiglumide
  • HY-19261
    T-0632
    		Antagonist 99.88%
    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-105257
    Pranazepide
    		Antagonist 99.81%
    Pranazepide (FR120480) is a selective cholecystokinin-1 receptor (CCK1-R) antagonist with an IC50 of 0.67 nM against CCK1-R. Pranazepide is applicable for the research of pancreatic diseases.
    Pranazepide
  • HY-101352
    LY 225910
    		Antagonist 98.92%
    LY 225910 is a selective antagonist for cholecystokinin receptor (CCK2 receptor), which affects the excitatory response to morphine, and leads to morphine sensitization.
    LY 225910
  • HY-148656
    PNB-001
    		Antagonist 99.65%
    PNB-001 is an orally active CCK2 selective ligand and antagonist. PNB-001 has anti-inflammatory and analgesic activities.
    PNB-001
  • HY-111313
    JNJ-26070109
    		Antagonist 99.25%
    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-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-106840A
    L-365260 hemihydrate
    		Antagonist 99.75%
    L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors.
    L-365260 hemihydrate
  • HY-118194
    A-65186
    		Antagonist 99.94%
    A-65186 is a CCK-A receptor antagonist with the activity of inhibiting CCK8-induced amylase secretion. A-65186 has high binding affinity for pancreatic CCK-A receptors, is more than 500 times more selective for CCK-A receptors than for CCK-B receptors, and can inhibit CCK8-induced amylase secretion.
    A-65186
  • HY-U00360
    (Rac)-Sograzepide
    		Antagonist 98.98%
    (Rac)-Sograzepide is an antagonist of cholecystokinin B (CCK-B) receptor, and has the potential of reducing the secretion of gastric acid.
    (Rac)-Sograzepide
  • HY-P5413
    [Lys3]-Bombesin
    		99.39%
    [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-105226B
    CI-988 hemihydrate
    		Antagonist ≥99.0%
    CI-988 hemihydrate (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 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects.
    CI-988 hemihydrate
  • 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-P0196A
    Cholecystokinin Octapeptide, desulfated TFA
    Cholecystokinin Octapeptide, desulfated (CCK Octapeptide, desulfated) TFA is a synthetic desulfated Cholecystokinin octapeptide (HY-P0093).
    Cholecystokinin Octapeptide, desulfated TFA
Cholecystokinin Receptor Isoform Comparison

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